Drug composition antagonistic to both PGD2/TXA2 receptors

ABSTRACT

A compound of the formula (I): 
                         
wherein A is alkylene optionally having an unsaturated bond; R is —C(═O)—R 1 ; R 1  is hydroxy or the like; m is 0 or 1; p is 0 or 1; X 1  and X 3  are each independently optionally substituted aryl or optionally substituted heteroaryl or the like; X 2  is a bond, —CH 2 —, —S—, —SO 2 —, —CH 2 —O—, —O—CH 2 —, —CH 2 —S—, —S—CH 2 —, or the like; X 4  is —CH 2 —, —CH 2 —CH 2 —, —C(═O)—, or the like, having a dual antagonistic activity against both a thromboxane A 2  receptor and a prostaglandin D 2  receptor is found.

This application is a U.S. national stage of International ApplicationNo. PCT/JP01/04430 filed May 28, 2001.

TECHNICAL FIELD

This invention relates to a pharmaceutical composition comprising a dualantagonist against thromboxane A₂ and prostagrandin D₂ receptors and indetail, a compound having a [2.2.1] or [3.1.1.] bicyclo skeleton.

BACKGROUND ART

As a pharmaceutical composition comprising a dual antagonist againstPGD₂/TXA₂ receptors, a compound of the formula:

wherein R^(X) is optionally substituted single ring or fusedheterocyclyl; X is hydrogen or alkyl, was described in WO 99/15502. Theabove mentioned compound has a substituent of the formula:—CH₂—CH═CH—CH₂—CH₂—CH₂—COOX wherein X is hydrogen or alkyl, as an αchain and R on an ω chain is a single or fused heterocycl optionallysubstituted with amino, halogen, hydroxy and the like.

Further, the other compounds having a [2.2.1] bicyclo skeleton similarto the compounds of the present invention have been described inWO97/00853 and the like. In this publication, it is described that thecompounds are useful as prostagrandin D₂ (PGD₂) antagonists.

However, in these publications, almost none of compound having othersubstituents than those represented by the formula:

wherein X¹ and X³ are each independently optionally substituted aryl,optionally substituted heteroaryl or optionally substituted non-aromaticheterocyclyl; X² is a bond, —CH₂—, —S—, —SO₂— and the like; X⁴ is —CH₂—and the like; m is 0 or 1; p is 0 or 1 as the ω chain, and furthermore,the formula: —CH₂—CH═CH—CH₂—CH₂—CH₂—COOR² wherein R² is hydrogen oralkyl, as the α chain of bicyclic ring, has been described.

PGD₂ receptor antagonists have a quite different character from that ofTXA₂ receptor antagonists in the site and mechanism of action andindications thereof.

On the other hand, a compound having a dual antagonistic activityagainst both a TXA₂ receptor and a PGD₂ receptor can be useful astherapeutic agents for various diseases caused by TXA₂ or PGD₂.

For example, in the case of bronchial asthma, it is known that TXA₂cause potent tracheal contraction and respiratory anaphylaxis and PGD₂effects infiltration of eosionophils. From these comprehension, TXA₂ andPGD₂ are thought to be one of causative substances of the pathopoiesisand advance of asthma, thus the dual antagonistic compounds are expectedto be more potent agents for treating asthma than ever knownantagonists.

Further, in the case of allergic rhinitis, it is recognized that TXA₂and PGD₂ cause the swelling of nasal mucosa through the aggravation ofvascular permeability, and PGD₂ induces the nasal blockage through theenlargement of vascular volume. Therefore, the dual antagonisticcompounds are expected to be more potent agents for treating nasalblockage than ever known antagonists.

These diseases and condition thereof might be treated by administeringboth a TXA₂ receptor antagonist and a PGD₂ receptor antagonist at thesame time, for example, in combination therapy or as a mixture thereof.But the administration of two or more agents often causes some problemsdue to the difference of their metabolic rate. For example, when theantagonists are different from each other in the time to reach a maximumblood concentration or the duration of action, they do not alwaysefficiently exhibit each receptor antagonistic effect at the same time,failing to give a desired additive or synergic effect.

It has therefore been desired to develop medicines having a dualantagonistic activity against TXA₂/PGD₂ receptors, which exhibit newexcellent therapeutic effects and can be used for many indications.

On the other hand, it was disclosed that 3-oxa-derivatives were preparedas metabolically stable TXA₂/PGH₂ receptor antagonists in Bioorganic &Medicinal Chemistry Letters, Vol.2, No.9, pp. 1069–1072, 1992. Theactive value of the compound was only described but the metabolicstability has not been described in the literature.

wherein, Z is p-fluorophenyl; Rω is benzenesulfonamino and the like.

Furthermore, it was reported in PROSTAGLANDINS, 1986, 31, 95 thatILOPROST, PGI₂ mimetics was stabilized metabolically by converting tothe 3-oxa-derivative. But, remaining activity of each compound was onlycompared under a presence of the metabolic enzyme of a rat and themetabolic stability did not mentioned, since there was a possibility ofa production of active metabolites

DISCLOSURE OF INVENTION

The present inventors have studied intensively to develop apharmaceutical composition having a dual antagonistic activity againstTXA₂/PGD₂ receptors and found out new compounds and pharmaceuticalcompositions comprising them.

The present invention provides:

-   (1) a compound of the formula (I):

wherein

-   -   A is alkylene optionally intervened with a heteroatom,        optionally having an oxo group, optionally substituted with        halogen and/or optionally having an unsaturated bond;    -   R is —C(═O)—R¹, —CH₂—R¹, or tetrazolyl;    -   R¹ is hydroxy, alkyloxy, or optionally substituted amino;    -   m is 0 or 1;    -   provided that combinations wherein m is 1, A is        —CH═CH—CH₂—CH₂—CH₂— and R is —C(═O)—R¹ (R¹ is hydroxy or        alkyloxy) and wherein A is —CH₂—CH═CH—CH₂—CH₂—CH₂— and R is        —C(═O)—R¹ wherein R¹ is hydroxy or alkyloxy are excluded, p is 0        or 1, provided when p=0, X¹ is not bonded to X³ via X⁴;    -   X¹ and X³ are each independently optionally substituted aryl,        optionally substituted heteroaryl or optionally substituted        non-aromatic heterocyclyl;    -   X² is a bond, —CH₂—, —CH₂—CH₂—, —C(═O)—, —O—, —S—, —SO—, —SO₂—,        —NH—, —N(CH₃)—, —C(═N—O—CH₃)—, —N═N—, —CH═CH—, —(C═O)—NH—,        —NH—(C═O)—, —CH₂—NH—, —NH—CH₂—, —CH₂—O—, —O—CH₂—, —CH₂—,        —S—CH₂—, —CH₂—SO₂—, —SO₂—CH₂—, —SO₂—NH—, —NH—SO₂—, —C(═CH₂)—,        —SO₂N(Me)—, —CH₂NHSO₂—, —CH₂NH—(C═O)—, —NH—C(═O)—NH or        —NH—C(═O)—N(Me)—;    -   X⁴ is —CH₂—, —CH₂—CH₂—, —C(═O)—, —SO—, —SO₂—, —(C═O)—NH—,        —NH—(C═O)—, —CH₂—NH—, —NH—CH₂—, —CH₂—O—, —O—CH₂—, —CH₂—S—,        —S—CH₂—, —CH₂—SO₂—, —SO₂—CH₂—, —SO₂—NH— or —NH—SO₂—,        provided that a combination wherein

-   -   A is —CH═CH—CH₂—CH₂—CH₂—, R is —COOH, m is 1, p is 0, X¹ and X³        are phenyl, and X² is —N═N—, is excluded        and provided that when

-   -   X¹ and X³ are phenyl, X² is —CH═CH—, —O—, or —S—, m is 0, and p        is 0, a compound wherein A is —CH═CH—CH₂—CH₂—CH₂—C(CH₃)₂— and R        is COOH, A is —CH₂—C(═O)—CH₂—CH₂—CH₂—CH₂— and R is COOH, A is        —CH₂—CH₂—CH₂—CH₂—CH₂— and R is —COOH, or A is        —CH═CH—CH₂—CH₂—CH₂— and R is —CH₂OH,        is excluded,        a prodrug, a pharmaceutically acceptable salt or a solvate        thereof,

-   (2) A compound as described in (1) wherein A is alkylene optionally    intervened with a heteroatom, optionally having an oxo group,    optionally substituted with halogen and/or optionally having a    unsaturated bond;    -   R is —C(═O)—R¹, —CH₂—R¹, or tetrazolyl;    -   R¹ is hydroxy, alkyloxy, or optionally substituted amino;    -   provided compounds wherein A is —CH═CH—CH₂—CH₂—CH₂— and R is        —C(═O)—R¹ (R¹ is hydroxy or alkyloxy), or A is        —CH₂—CH═CH—CH₂—CH₂—CH₂— and R is —C(═O)—R¹ wherein R¹ is hydroxy        or alkyloxy are excluded,        a prodrug, a pharmaceutically acceptable salt or a solvate        thereof,

-   (3) A compound as described in (1) or (2), wherein A is alkylene    intervened with a heteroatom, optionally having an oxo group,    optionally substituted with halogen and/or optionally having an    unsaturated bond,    a prodrug, a pharmaceutically acceptable salt, or a solvate thereof,

-   (4) A compound as described in (1) or (2), wherein A is C1 to C4 or    C7 to C9 alkylene optionally intervened with a heteroatom,    optionally having an oxo group, optionally substituted with halogen    and/or optionally having an unsaturated bond, a prodrug, a    pharmaceutically acceptable salt, or a solvate thereof,

-   (5) A compound as described in (1) or (2), wherein A is    —CH₂—CH₂—CH₂—, —CH₂—CH₂—CH(F)—, —CH₂CH═CH—, —CH₂—O—CH₂—,    —CH₂CH═C(F)—, —CH₂—CH₂—CH₂—CH₂—, —CH₂CH═CH—CH₂—, —CH₂—CH₂—CH═CH—,    —CH═CH—CH₂—CH₂—, —CH₂—CH₂—O—CH₂—, —CH₂—CH₂—S—CH₂—, —CH₂—CO—NH—CH₂—,    —CH₂—CH₂—CH₂—CH₂—CH₂—, —CH₂CH═CH—CH₂—CH₂—, —CH₂ 13 CH₂—CH₂—CH═CH—,    —CH₂—CH₂—CH₂—O—CH₂—, —CH₂—CH₂—CH₂—S—CH₂—, —CH₂—CH₂—CO—NH—CH₂—,    —CH₂—CH₂—CH₂—CH₂—CH₂—CH₂—, —CH₂—CH₂—CH₂—CH₂—CH₂—CH(Me)—,    —CH₂—CH₂—CH₂—CH₂—CH₂—C(Me)₂—, —CH₂—CH₂—CH₂—CH₂—CH₂—CH(F)—,    —CH₂—CH═CH—CH₂—CH₂—CH(Me)—, —CH₂—CH═CH—CH₂—CH₂—C(Me)₂—,    —CH₂—CH═CH—CH₂—CH₂—CH(F)—, —CH₂—CH₂—CH₂—CH₂—CH═CH—,    —CH₂—CH₂—CH₂—CH₂—CH═C(Me)—, —CH₂—CH₂—CH₂—CH₂—C(Me)═CH—,    —CH₂—CH₂—CH₂—CH₂—CH═C(F)—, —CH₂—CH₂—CH₂—CH₂—O—CH₂—,    —CH₂—CH═CH—CH₂—O—CH₂—, —CH₂—CH═CH—CH₂—S—CH₂—,    —CH₂—CH═C(F)—CH₂—O—CH₂—, —CH₂—CH₂—O—CH₂—CH═CH—,    —CH₂—CH₂—CH₂—CH₂—S—CH₂—, —CH₂—CH₂—CH₂—CO—NH—CH₂—,    —CH₂—CH₂CH═N—O—CH₂—, —CH₂—CH₂—S—CH₂—CH₂—CH₂—,    —CH₂—CH₂—CH₂—CH₂—CH₂—CH₂—CH₂—, —CH₂—CH═CH—CH₂—CH₂—CH₂—CH₂—,    —CH₂—CH₂—CH₂—CH₂—CH₂—O—CH₂—, —CH₂—CH₂—CH₂—CH₂—CH₂—CH₂—CH₂—, or    —CH₂—CH═CH—CH₂—CH₂—CH₂—CH₂—CH₂—,    a prodrug, a pharmaceutically acceptable salt, or a solvate thereof,

-   (6) A compound as described in (5), wherein A is —CH₂—CH₂—CH₂—CH₂—,    —CH₂—CH₂—CH₂—CH₂—CH═CH—, —CH₂—CH₂—CH₂—CH₂—O—CH₂—,    —CH₂—CH═CH—CH₂—O—CH₂—, —CH₂—CH═CH—CH₂—S—CH₂—, or    —CH₂—CH₂—CH₂—CH₂—S—CH₂—,    a prodrug, a pharmaceutically acceptable salt, or a solvate thereof,

-   (7) A compound as described in (6), wherein A is    —CH₂—CH₂—CH₂—CH₂—O—CH₂—,    a prodrug, a pharmaceutically acceptable salt, or a solvate thereof,

-   (8) A compound as described in any one of (1) to (7), wherein X¹ and    X³ are each independently optionally substituted aryl or optionally    substituted heteroaryl,    a prodrug, a pharmaceutically acceptable salt, or a solvate thereof,

-   (9) A compound as described in (8), wherein at least one of X¹ and    X³ is optionally substituted heteroaryl,    a prodrug, a pharmaceutically acceptable salt, or a solvate thereof,

-   (10) A compound as described in (9), wherein X¹ and X³ are each    independently optionally substituted heteroaryl,    a prodrug, a pharmaceutically acceptable salt, or a solvate thereof,

-   (11) A compound as described in (9), wherein at least one of X¹ and    X³ is optionally substituted thienyl or optionally substituted    benzothienyl,    a prodrug, a pharmaceutically acceptable salt, or a solvate thereof,

-   (12) A compound as described in any one of (1) to (11), wherein X²    is a bond, —CH₂—, —S—, —SO₂—, —CH₂—O—, —O—CH₂—, —CH₂—S—, —S—CH₂—, or    —NH—C(═O)—NH—,    a prodrug, a pharmaceutically acceptable salt, or a solvate thereof,

-   (13) A compound as described in any one of (1) to (12), wherein m is    0 and p is 0,    a prodrug, a pharmaceutically acceptable salt, or a solvate thereof,

-   (14) A compound as described in any one of (1) to (13), wherein R is    —C(═O)—R¹ and R¹ is hydroxy, alkyloxy, or optionally substituted    amino,    a prodrug, a pharmaceutically acceptable salt, or a solvate thereof,

-   (15) A pharmaceutical composition containing a compound, a prodrug,    a pharmaceutically acceptable salt, or a solvate thereof as    described in any one of above (1) to (14),

-   (16) A pharmaceutical composition having a dual antagonistic    activity against PGD₂/TXA₂ receptors as described in the above (15),

-   (17) A pharmaceutical composition as described in the above (15),    which is used for treatment of asthma,

-   (18) A pharmaceutical composition as described in the above (15),    which is used for the treatment of nasal blockage,

-   (19) A pharmaceutical composition as described in the above (15),    which is used for the treatment of allergic conjunctivitis,

-   (20) A pharmaceutical composition as described in the above (15),    which is used for the treatment of allergic rhinitis,

-   (21) Use of the compound as described in any one of (1) to (14) for    the preparation of a pharmaceutical composition for treating asthma,    nasal blockage, allergic conjunctivitis or allergic rhinitis,

-   (22) A method for treating nasal blockage, allergic conjunctivitis    or allergic rhinitis, which comprises administrating a compound as    described in any one of (1) to (14),

-   (23) A compound of formula: X³—X²—X¹—COOH wherein X³ is pyrrolyl    optionally substituted with alkyl, alkyloxy or halogen, indolyl    optionally substituted with alkyl, alkyloxy or halogen, indolinyl    optionally substituted with alkyl, alkyloxy or halogen, or    1,2,3,4-tetrahydroquinolyl optionally substituted with alkyl,    alkyloxy or halogen; X² is —SO₂—, —S— or —CH₂—; X¹ is thienyl, or a    salt thereof,

-   (24) A compound as described in (23), wherein a substituent of the    formula: —X¹—X²—X³ is 5-(1-pyrrolylsulfonyl)thiophen-2-yl,    5-[(2-methyl-1-pyrrolyl)sulfonyl]thiophen-2-yl, or    5-[(2,5-dimethyl-1-pyrrolyl)sulfonyl]thiophen-2-yl, or a salt    thereof.

BEST MODE FOR CARRYING OUT THE INVENTION

Special feature of a compound in the present invention is

-   -   (A) a bicyclic ring represented by the Y ring of the above        formula (I) is [2.2.1] or [3.1.1] skeleton,    -   (B) an ω chain attached to the bicyclic ring, a group        represented by the formula:

-   -    of the above formula (I), includes —NH—CO—, and X¹ and X³ are        each independently optionally substituted aryl, optionally        substituted heteroaryl or optionally substituted non-aromatic        heterocyclyl;    -   (C) X¹ bonds to X³ via X²,    -   (D) an α chain is represented by the formula: —A—R, wherein A is        alkylene optionally intervened with a heteroatom, optionally        having an oxo group, optionally substituted with halogen and/or        optionally having an unsaturated bond; R is —C(═O)—R¹, —CH₂—R¹,        or tetrazolyl; R¹ is hydroxy, alkyloxy, or optionally        substituted amino, and the like.

Provided that a compound wherein A is —CH₂—CH═CH—CH₂—CH₂—CH₂— and R is—C(═O)—R¹ (R¹ is hydroxy or alkyloxy), is not included in the presentinvention, since the compound is metabolically unstable coused byoxidizaton of an α-chain at β-position.

Therefore, a compound of the present invention has a special feature atA and R and has an improved metabolic property. Further, a compound ofthe present invention is a dual antagonistic activity against PGD₂/TXA₂receptors having the above mentioned features (A) to (D).

A preferred embodiment is a compound of the formula (I) wherein

-   -   (1) X¹ and X³ are each independently optionally substituted aryl        or optionally substituted heteroaryl,    -   (2) at least one of X¹ and X³ is optionally substituted        heteroaryl,    -   (3) X¹ and X³ are each independently optionally substituted        heteroaryl,    -   (4) at least one of X¹ and X³ is optionally substituted thienyl        or optionally substituted benzothienyl,    -   (5) X² is a bond, —CH₂—, —S—, —SO₂—, —CH₂—O—, —O—CH₂—, —CH₂—S—,        —S—CH₂— or —NH—C(═O)—NH—,    -   (6) m is 0 and p is 0,    -   (7) R is —C(═O)—R¹, wherein R¹ is hydroxy, alkyloxy or        optionally substituted amino,    -   (8) in a case of a combination of any one of (1) to (4) with        (5),    -   (9) in a case of a combination of any one of (1) to (4) with        (6),    -   (10) in a case of a combination of any one of (1) to (4) with        (7).

Each term used herein is defined to have meanings below in either caseof a single or a joint use with other terms, unless otherwise noted.

“Alkylene” used herein means a straight chain and branched chain C1 toC9 and refers to methylene, methylmethylene, dimethylmethylene,ethylmethylmethylene, ethylene, trimethylene, tetramethylene,pentamethylene, hexamethylene, heptamethylene, octamethylene,nonamethylene, and the like. The above mentioned alkylene optionallycontains a hetero atom (oxygen atom, sulfur, nitrogen atom or the like),optionally has an oxo group (═O), is optionally substituted with halogen(e.g. F, Cl, Br, I, preferable is F) and/or optionally contains one ormore unsaturated bond (double bond or triple bond) on the chain at anyposition. Examples are —CH₂—CH₂—CH₂—, —CH₂—CH₂—CH(F)—, —CH₂—CH═CH—,—CH₂—O—CH₂—, —CH₂—CH═C(F)—, —CH₂—CH₂—CH₂—CH₂—, —CH₂—CH═CH—CH₂—,—CH₂—CH₂—CH═CH—, —CH═CH—CH₂—CH₂—, —CH₂—CH₂—O₂—CH₂—, —CH₂—CH₂—S—CH₂—,—CH₂—CO—NH—CH₂—, —CH₂—CH₂—CH₂—CH₂—CH₂—, —CH₂—CH═CH—CH₂—CH₂—,—CH₂—CH₂—CH₂—CH═CH—, —CH═CH—CH₂—CH₂—CH₂—, —CH₂—CH₂—CH₂—O—CH₂—,—CH₂—CH₂—CH₂—S—CH₂—, —CH₂—CH₂—CO—NH—CH₂—, —CH₂—CH₂—CH₂—CH₂—CH₂—CH₂—,—CH₂—CH₂—CH₂—CH₂—CH₂—CH(Me)—, —CH₂—CH₂—CH₂—CH₂—CH₂—C(Me)₂—,—CH₂—CH₂—CH₂—CH₂—CH₂—CH(F)—, —CH₂—CH═CH—CH₂—CH₂—CH₂—,—CH₂—CH═CH—CH₂—CH₂—CH(Me)—, —CH₂—CH═CH—CH₂—CH₂—C(Me)₂—,—CH₂—CH═CH—CH₂—CH₂—CH(F)—, —CH₂—CH₂—CH₂—CH₂—CH═CH—,—CH₂—CH₂—CH₂—CH₂—CH═C(Me)—, —CH₂—CH₂—CH₂—CH₂—C(Me)═CH—,—CH₂—CH₂—CH₂—CH₂—CH═C(F)—, —CH₂—CH₂—CH₂—CH₂—O—CH₂—,—CH₂—CH═CH—CH₂—O—CH₂—, —CH₂—CH═CH—CH₂—S—CH₂—, —CH₂—CH═C(F)—CH₂—O—CH₂—,—CH₂—CH₂—O—CH₂—CH═CH—, —CH₂—CH₂—CH₂—CH₂—S—CH₂—, —CH₂—CH₂—CH₂—CO—NH—CH₂—,—CH₂—CH₂—CH═N—O—CH₂—, —CH₂—CH₂—S—CH₂—CH₂—CH₂—,—CH₂—CH₂—CH₂—CH₂—CH₂—CH₂—CH₂—, —CH₂—CH═CH—CH₂—CH₂—CH₂—CH₂—,—CH₂—CH₂—CH₂—CH₂—CH₂—O—CH₂—, —CH₂—CH₂—CH₂—CH₂—CH₂—CH₂—CH₂—CH₂—,—CH₂—CH═CH—CH₂—CH₂—CH₂—CH₂—, —CH₂—CH₂—O—CH₂—CH₂—CH₂—,—CH₂—CH═CH—CH₂—CH═CH₂—, and the like.

Especially, the following embodiment is preferred for the abovementioned “alkylene”:

-   -   1) alkylene intervened with a heteroatom, optionally having an        oxo group, optionally substituted halogen and/or optionally        containing unsaturated bond(s),    -   2) C1 to C4 or C7 to C9 alkylene optionally intervened with a        heteroatom, optionally having an oxo group, optionally        substituted halogen and/or optionally containing unsaturated        bond(s),    -   3) —CH₂—CH₂—CH₂—, —CH₂—CH₂—CH(F)—, —CH₂—CH═CH—, —CH₂—O—CH₂—,        —CH₂—CH₂—CH(F)—, —CH₂—CH₂—CH₂—CH₂—, —CH₂—CH═CH—CH₂—,        —CH₂—CH₂—CH═CH—, —CH═CH—CH₂—CH₂—, —CH₂—CH₂—O₂—CH₂—,        —CH₂—CH₂—S—CH₂—, —CH₂—CO—NH—CH₂—, —CH₂—CH₂—CH₂—CH₂—CH₂—,        —CH₂—CH═CH—CH₂—CH₂—, —CH₂—CH₂—CH₂—CH═CH—, —CH₂—CH₂—CH₂—O—CH₂—,        —CH₂—CH₂—CH₂—S—CH₂—, —CH₂—CH₂—CO—NH—CH₂—,        —CH₂—CH₂—CH₂—CH₂—CH₂—CH₂—, —CH₂—CH₂—CH₂—CH₂—CH₂—CH(Me)—,        —CH₂—CH₂—CH₂—CH₂—CH₂—C(Me)₂—, —CH₂—CH₂—CH₂—CH₂—CH₂—CH(F)—,        —CH₂—CH═CH—CH₂—CH₂—CH(Me)—, —CH₂—CH═CH—CH₂—CH₂—C(Me)₂—,        —CH₂—CH═CH—CH₂—CH₂—CH(F)—, —CH₂—CH₂—CH₂—CH₂—CH═CH—,        —CH₂—CH₂—CH₂—CH₂—CH═C(Me)—, —CH₂—CH₂—CH₂—CH₂—C(Me)═CH—,        —CH₂—CH₂—CH₂—CH₂—CH═C(F)—, —CH₂—CH₂—CH₂—CH₂—O—CH₂—,        —CH₂—CH═CH—CH₂—O—CH₂—, —CH₂—CH═CH—CH₂—S—CH₂—,        —CH₂—CH═C(F)—CH₂—O—CH₂—, —CH₂—CH₂—O—CH₂—CH═CH—,        —CH₂—CH₂—CH₂—CH₂—S—CH₂—, —CH₂—CH₂—CH₂—CO—NH—CH₂—,        —CH₂—CH₂—CH═N—O—CH₂—, —CH₂—CH₂—S—CH₂—CH₂—CH₂—,        —CH₂—CH₂—CH₂—CH₂—CH₂—CH₂—CH₂—, —CH₂—CH═CH—CH₂—CH₂—CH₂—CH₂—,        —CH₂—CH₂—CH₂—CH₂—CH₂—O—CH₂—, —CH₂—CH₂—CH₂—CH₂—CH₂—CH₂—CH₂—CH₂—,        or —CH₂CH═CH—CH₂—CH₂—CH₂—CH₂—CH₂—,    -   4) —CH₂—CH₂—CH₂—CH₂—, —CH₂—CH₂—CH₂—CH₂—CH═CH—,        —CH₂—CH₂—CH₂—CH₂—O—CH₂—, —CH₂—CH═CH—CH₂—O—CH₂—,        —CH₂—CH═CH—CH₂—O—CH₂—, or —CH₂—CH₂—CH₂—CH₂—S—CH₂—, and    -   5) —CH₂—CH₂—CH₂—CH₂—O—CH₂—.

The term “heteroaryl” includes a group which has a bond at anysubstitutable and which can be converted from a 5- to 7-memberedaromatic heterocycle containing one or more oxygen atom, sulfur atomand/or nitrogen atom in the ring, or such an aromatic heterocycle asfused with one or more carbocycle or other aromatic heterocycle. Any oneof aromatic heterocycle and aromatic carbocycle may have a bond.“Heteroaryl” may have a bond at a nitrogen atom as well as a carbon atomof aromatic heterocycle or aromatic carbocycle. Examples of “heteroaryl”include pyrrolyl (e.g., 1-pyrrolyl, 2-pyrrolyl, 3-pyrrolyl), pyridyl(e.g., 2-pyridyl, 3-pyridyl, 4-pyridyl), pyrazolyl (e.g., 1-pyrazolyl,3-pyrazolyl, 4-pyrazolyl), imidazolyl (e.g., 1-imidazolyl, 2-imidazolyl,4-imidazolyl), pyrimidinyl (e.g., 2-pyrimidinyl, 4-pyrimidinyl,5-pyrimidinyl), pyrazinyl (e.g., 2-pyrazinyl), indolyl (e.g., 1-indolyl,2-indolyl, 3-indolyl, 4-indolyl, 5-indolyl, 6-indolyl, 7-indolyl),carbazolyl (e.g., 1-carbazolyl, 2-carbazolyl, 3-carbazolyl,4-carbazolyl, 9-carbazolyl), benzimidazolyl (e.g., 1-benzimidazolyl,2-benzimidazolyl, 4-benzimidazolyl, 5-benzimidazolyl), indazolyl (e.g.,1-indazolyl, 2-indazolyl, 3-indazolyl, 4-indazolyl, 5-indazolyl,6-indazolyl, 7-indazolyl), quinolyl (e.g., 2-quinolyl, 3-quinolyl,4-quinolyl, 5-quinolyl, 6-quinolyl, 7-quinolyl, 8-quinolyl), isoquinolyl(e.g., 1-isoquinolyl, 3-isoquinolyl, 4-isoquinolyl, 5-isoquinolyl,6-isoquinolyl, 7-isoquinolyl, 8-isoquinolyl), furyl (e.g., 2-furyl,3-furyl), benzofuryl (e.g., 2-benzofuryl, 3-benzofuryl, 4-benzofuryl,5-benzofuryl, 6-benzofuryl, 7-benzofuryl), thienyl (e.g., 2-thienyl,3-thienyl), benzothienyl (e.g., benzo[b]thiophen-2-yl,benzo[b]thiophen-3-yl, benzo[b]thiophen-4-yl, benzo[b]thiophen-5-yl,benzo[b]thiophen-6-yl, benzo[b]thiophen-7-yl), dibenzothienyl (e.g.,2-dibenzothienyl, 3-dibenzothienyl), dibenzofuryl (e.g., 2-dibenzofuryl,3-dibenzofuryl), naphthothienyl (e.g., naphtho[2,3-b]thiophen-2-yl,naphtho[2,3-b]thiophen-3-yl, naphtho[1.2-b]thiophen-2-yl,naphtho[1.2-b]thiophen-3-yl), oxazolyl (e.g., 2-oxazolyl, 4-oxazolyl,5-oxazolyl), isoxazolyl (e.g., 3-isoxazolyl, 4-isoxazolyl,5-isoxazolyl), thiazolyl (e.g., 2-thiazolyl, 4-thiazolyl, 5-thiazolyl),isothiazolyl (e.g., 3-isothiazolyl, 4-isothiazolyl, 5-isothiazolyl),imidazothiazolyl (e.g., imidazo[2.1-b]thiazol-2-yl,imidazo[2.1-b]thiazol-3-yl), benzoisoxazolyl (e.g.,benzo[d]isoxazol-3-yl), benzothiazolyl (e.g., benzo[d]thiazol-2-yl), andthe like.

The term of “aromatic carbocycle or other aromatic heterocycle” whichmay fuse the above “heteroaryl” includes 5- to 7-membered aromatic cyclewhich may contains one or more oxygen atom, sulfur atom and/or nitrogenatom in the ring, or such an aromatic ring as fused with one or moreother aromatic rings.

The term of “aryl” includes mono aromatic carbocyclyl (e.g., phenyl) orfused aromatic carbocyclyl (e.g., 1-naphthyl, 2-naphthyl, 1-anthryl,9-anthryl, 1-phenanthryl, 10-phenanthryl).

The term of “non-aromatic heterocyclyl” includes a group which has abond at any substitutable and which can be converted from 3- to7-membered non-aromatic heterocyclyl which contains one or more oxygenatom, sulfur atom and/or nitrogen atom in the ring, or non-aromaticheterocyclyl which is fused with a carbon ring (e.g. aromaticcarbocycle) or other heterocyclyl (e.g. aromatic heterocycle). Thesubstitutable bond may exist not only on the carbon atom but also on thenitrogen atom in the non-aromatic heterocyclyl. Examples are aziridinyl,piperidino, piperidinyl, morphorino, morphorinyl, pyrrolinyl,pyrrolidinyl, imidazolinyl, piperadino, piperadinyl, isooxazolinyl,thiolanyl, tetrahydrofuranyl, dioxanyl, oxathianyl, tetrahydropyranyl,and the like. Preferable is 5- or 6-membered non-aromatic heterocyclylcontaining a nitrogen atom. The following groups are exexplified as agroup which has a bond at any substitutable and which can be convertedfrom non-aromatic heterocyclyl fused with one or more carbon ring (e.g.aromatic carbocycle) or other heterocyclyl (e.g. aromatic heterocycle):

Furthermore, the substitutable bond may exist at any position of thecarbon atom or the nitrogen atom.

“Aryl” or “heteroaryl” may be fused 4- to 7-membered cycloalkane or 4-to 7-membered non-aromatic heterocycle. Examples of cycloalkane includecyclobutane, cyclopentane, cyclohexane, and cycloheptane. Examples ofnon-aromatic heterocycle include pyrrolidine, piperazine, oxorane,1,3-dioxorane, 1,4-dioxane, thiorane, or the like. The above“cycloalkane” and “non-aromatic heterocycle” may be fused with otheraromatic carbocycle or aromatic heterocycle. Examples of aryl orheteroaryl fused with 4- to 7-membered cycloalkane or 4- to 7-memberednon-aromatic heterocycle are illustrated below.

Examples of the substituent on “optionally substituted aryl”,“optionally substituted heteroaryl” or “optionally substitutednon-aromatic heterocyclyl” include a group of the formula: —Z¹—Z²wherein Z¹ is a bond, —O—, —S—, —NH—, —NH—C(═O)—, —NH—C(═O)—O—,—NH—SO₂—, —C(═O)—, —O—C(═O)—, —C(═O)—O—, or —SO₂—; and Z² is alkyl,haloalkyl, alkenyl, alkynyl, aryl optionally substituted with alkyl orhalogen, heteroaryl optionally substituted with alkyl or halogen,arylalkyl optionally substituted with alkyl or halogen, heteroarylalkyloptionally substituted with alkyl or halogen, carboxy, halogen (F, Cl,Br, I), hydroxyalkyl, hydroxy, nitro, cyano, mercapto, thioformyl,thioacetyl, thiocarboxy, dithiocarboxy, thiocarbamoyl, sulfino, sulfo,sulfamoyl, sulfoamino, optionally substituted amino, optionallysubstituted aminoalkyl, hydroxyamino, carbamoyl, or hydorazino. One tothree substituents may be at any suitable position on the above aryl,heteroaryl, or non-aromatic heterocyclyl.

“Alkyl” includes a straight or branched C1 to C8 alkyl group or a C3 toC8 cycloalkyl group. Examples are methyl, ethyl, n-propyl, isopropyl,n-butyl, isobutyl, tert-butyl, n-pentyl, isopentyl, n-hexyl, n-heptyl,n-octyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyland the like.

“Haloalkyl” includes a straight or branched C1 to C8 alkyl or C3 to C8cycloalkyl group substituted with one or more halogen, for example,chloromethyl, fluoromethyl, trifluoromethyl, 2,2,2-trifluoroethyl,1,1-difluoroethyl, trichloromethyl, 2,2,2-trichloroethyl,1,1-dichloroethyl or the like.

“Alkenyl” includes a straight or branched C2 to C8 alkenyl or C3 to C8cycloalkenyl group having one or more double bond(s), for example,vinyl, 1-propenyl, 2-propenyl, isopropenyl, 2-cyclobuten-1-yl,2-cyclopenten-1-yl, 3-cyclopenten-1-yl, 2-cyclohexen-1-yl or the like.

“Alkynyl” includes a straight or branched C2 to C8 alkynyl having one ormore triple bond(s), for example, ethynyl, 1-propynyl, 2-propynyl,1-butynyl, 2-butynyl, 3-butynyl or the like.

“Halogen” includes fluoro, chloro, bromo, and iodo.

“Alkyl” used in the term “arylalkyl” or “heteroarylalkyl” have the samemeaning of the above “alkyl”, “aryl” used in the term “arylalkyl” havethe same meaning of the above “aryl” and “heteroaryl” used in the term“heteroarylalkyl” have the same meaning of the above “heteroaryl”.

“Hydroxy alkyl” includes the above “alkyl” substituted with one or twohydroxy, for example, hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl,1,2-dihydroxyethyl, 1,2-dihydroxy-n-propyl or the like.

Examples of the substituent of “optionally substituted amino” or“optionally substituted amino alkyl” include the above “alkyl”, theabove “arylalkyl”, the above “aryl”, the above “heteroaryl”, the above“heteroarylalkyl” hydroxy. Alkylsulfonyl, or the like. They may be mono-or di-substituted with these substituents. When the substituent isalkyl, alkyl may form a ring together with a nitrogen atom of an aminogroup.

Example of “optionally substituted amino” includes amino,N,N-dimethylamino, N-ethyl-N-methylamino, N,N-(diethylamino,pyrrolidino, piperidino, N-methyl-N-phenylamino, isopropylamino,diisopropylamino, hydroxyamino, alkylsulfonylamino (e.g.,methanesulfonylamino, ethanesulfonylamino, etc.), arylsulfonyl (e.g.,benzenesulfonylamino, toluenesulfonylamino, etc.),N-alkyl-N-alkylsulfonylamino (e.g., N-methyl-N-methanesulfonylamino,etc.), halogenated alkylsulfonylamino (e.g.,trifluoromethanesulfonylamino, etc.), or the like.

Examples of “optionally substituted aminoalkyl” includeN,N-dimethylaminomethyl, N-ethyl-N-methylaminomethyl,N,N-diethylaminomethyl, pyrrolidinomethyl, piperidinomethyl,N-methyl-N-phenylaminomethyl, isopropylaminomethyl,diisopropylaminomethyl or the like.

“A pharmaceutical composition having a dual antagonistic activityagainst PGD₂/TXA₂ receptors” means a pharmaceutical compositioncomprising at least one compound of the formula (I) having anantagonistic activity against both a PGD₂ receptor and a TXA₂ receptor.In addition to a compound of the formula (I), the other active agents(e.g. antiinflammatory agents, antiallergy agents and the like) andpharmaceutically acceptable admixtures (e.g., binding agent, filler andthe like) may be included.

The compound of the present invention has an antagonistic activityagainst PGD₂ receptor and TXA₂ receptor and can exhibit antagonisticactivities against PGD₂ receptor and TXA₂ receptor in vivo. For example,even if a compound has both antagonistic activities against receptors invitro, the compound administered can not always exhibit both of theantagonistic activity in vivo, owing to the preferential binding to thereceptor of stronger affinity. Therefore, as a compound of the presentinvention, preferable is that the compound has antagonistic activitiesagainst PGD₂ and TXA₂ receptors and is 100 times, preferably 50 time andmore preferably ca. 10 times in a ratio between affinities against PGD₂and TXA₂ receptors. The ratio between affinities against PGD₂ and TXA₂receptors can be calculated by the use of IC₅₀ values and the like.

Furthermore, as a compound of the present invention, preferable is lessthan 0.1 μM in the binding activity against TXA₂ receptor using humanplatelet membrane (IC₅₀ value) and 0.1 μM in the antagonistic activityagainst PGD₂ receptor using human platelet (IC₅₀ value). In particular,the compound is preferable, in which both of the binding activityagainst TXA₂ receptor using human platelet membrane (IC₅₀ value) and theantagonistic activity against PGD₂ receptor using human platelet (IC₅₀value) are less than 0.1 μM. Furthermore, the compound is preferable, inwhich their ratio is 100 times, preferably 50 time and more preferablyca. 10 times.

The present invention includes a method for treating asthma, nasalblockage, allergic conjunctivitis or allergic rhinitis which comprisesadministering a compound of the formula (I) and use of a compound of theformula (I) for manufacturing a medicine for asthma, nasal blockageallergic conjunctivitis or allergic rhinitis.

Furthermore, in a compound displayed in formula (I), “α chain” means agroup represented by the formula: —A—R¹, and “ω chain” means a grouprepresented by the formula:

Preferable is following substituents as the α chain. Furthermore, E andZ mean E-form and Z-form in double bond of each formula, respectively.Each sign in 4A to 9B means an A part of the formula and means the samegroup in Table 1 to Table 15 in this description.

4A —CH₂CH₂CH₂—R 4B —CH₂CH₂CH(F)—R 4C

4D

4E —CH₂OCH₂—R 5A —CH₂CH₂CH₂CH₂—R 5B

5C

5D

5E —CH₂CH₂OCH₂—R 5F —CH₂CH₂SCH₂—R 5G —CH₂CONHCH₂—R 6A —CH₂CH₂CH₂CH₂CH₂—R6B

6C

6D

6E —CH₂CH₂CH₂OCH₂—R 6F —CH₂CH₂CH₂SCH₂—R 6G —CH₂CH₂CONHCH₂—R 7A—CH₂CH₂CH₂CH₂CH₂CH₂—R 7B —CH₂CH₂CH₂CH₂CH₂CH(Me)—R 7C—CH₂CH₂CH₂CH₂CH₂C(Me)₂—R 7D —CH₂CH₂CH₂CH₂CH₂CH(F)—R 7E

7F

7G

7H

7I

7J

7K

7L

7M —CH₂CH₂CH₂CH₂OCH₂—R 7N

7O

7P

7Q

7R —CH₂CH₂CH₂CH₂SCH₂—R 7S —CH₂CH₂CH₂CONHCH₂—R² 7T —CH₂CH₂CH═N—OCH₂—R² 7U—CH₂CH₂SCH₂CH₂CH₂—R² 7V

8A —CH₂CH₂CH₂CH₂CH₂CH₂CH₂—R² 8B

8C —CH₂CH₂CH₂CH₂CH₂OCH₂—R² 9A —CH₂CH₂CH₂CH₂CH₂CH₂CH₂CH₂—R² 9B

R is exemplified by —C(═O)—R¹, —CH₂—R¹, or tetrazolyl and preferable is—C(═O)—R¹, wherein, R¹ is hydroxy, alkyloxy, or optionally substitutedamino. Examples of R are COOH, COOMe, CONH₂, CONHSO₂Me, CH₂OH, CH₂OMe,CONHMe, CON(Me)SO₂Me, 5-tetrazolyl, CONHSO₂Ph, CONHSO₂CF₃ and the like.

Furthermore, the combination of A and R includes all of the combinationand preferable is a combination described in Table 1 to Table 15.

As an ω chain, the following embodiments are preferred in the formula:

-   -   1) wherein m is 0 and p is 0,    -   2) wherein X¹ and X³ are each independently optionally        substituted aryl or optionally substituted heteroaryl,    -   3) wherein at least one of X¹ and X³ is optionally substituted        heteroaryl,    -   4) wherein X¹ and X³ are each independently optionally        substituted heteroaryl,    -   5) wherein at least one of X¹ and X³ is optionally substituted        thienyl or optionally substituted benzothienyl,    -   6) wherein X² is a bond, —CH₂—, —S—, —SO₂—, —CH₂—O—, —O—CH₂—,        —CH₂—S—, —S—CH₂—, or NH—C(═O)—NH—.

Concretely, preferable is a combination described below for the formula:—X¹—X²—X³. Furthermore, each sign of 1 to 513 below means a group shownby the formula: —X¹—X²—X³ and the compound number both in Table 1 toTable 15 and in Examples of reference in the present invention means thesame group.

—X¹—X²—X³ 1

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A compound of the present invention can be any of the following stereoisomers of [2.2.1] and [3.1.1] bicyclic skeleton.

In these stereo isomers, preferable is a compound having the skeleton ofthe formula:

The present invention includes all stereo isomers of them and theoptional mixtures thereof. Namely, the bond binding to the bicyclic ringis in R configuration or S configuration, and all of the stereo isomers(diastereomer, epimer, enantiomer and the like), racemates, and optionalmixture thereof are included in the present invention.

Moreover, the α chain of the compound of the present invention can be inZ configuration or E configuration, thus a compound having any of theconfigurations and the mixture thereof are included in the presentinvention.

A prodrug of a compound of the formula (I) is a derivative of thecompound of the present invention having a group which can be decomposedchemically or metabolically, and such prodrug is converted to apharmaceutically active compound of the present invention by means ofsolvolysis or by placing the compound in vivo under a physiologicalcondition. Method for the selection and process of an appropriateprodrug derivative are described in the literature such as Design ofProdrugs, Elsevier, Amsterdam 1985.

When the compound of the formula (I) has a carboxyl group, an esterderivative prepared by reacting a basal acid compound with a suitablealcohol or an amide derivative prepared by reacting a basal acidcompound with a suitable amine is exemplified as a prodrug. Aparticularly preferred ester derivative as an prodrug is an optionallysubstituted alkyl ester derivative (e.g., methyl ester, ethyl ester,n-propyl ester, isopropyl ester, n-butyl ester, isobutyl ester,tert-butyl ester, morpholinoethyl ester), an arylalkyl ester derivative(e.g., benzyl ester, phenethyl ester, benzhydryl ester), or the like. Aparticularly preferred amide derivative as a prodrug is alkyl amidederivative (e.g., N-methyl amide, N-ethyl amide, N-(n-propyl)amide,N-isopropyl amide, N-(n-butyl)amide, N-isobutyl amide,N-(tert-butyl)amide), aryl alkyl amide (e.g., N-benzyl amide,N-phenethyl amide, benzhydryl amide), or the like.

When the compound of the formula (I) has a hydroxy group, an acyloxyderivative prepared by reacting with a suitable acyl halide (e.g., acidchloride, halogenated acid) or a suitable acid anhydride (e.g., mixedacid anhydride) is exemplified as a prodrug. A particularly preferredacyloxy derivative as a prodrug is a derivative substituted withoptionally substituted alkylcarbonyloxy (e.g., —OCOC₂H₅, —OCO(tert-Bu),—OCOC₁₅H₃₁, —OCOCH₂CH₂COONa, —OCOCH(NH₂)CH₃, —OCOCH₂N(CH₃)₂—),optionally substituted arylcarbonyloxy (e.g., —OCO(m-COONa-Ph) or thelike.

When the compound of the formula (I) has an amino group, an amidederivative prepared by reacting with a suitable acid halide or asuitable acid anhydride is exemplified as a prodrug. A particularlypreferred amide derivative as a prodrug is a derivative substituted withoptionally substituted alkylcarbonyl (e.g., —NHCO(CH₂)₂₀CH₃,—NHCOCH(NH₂)CH₃) or the like.

Examples of a salt of the compound of the formula (I) or its prodruginclude alkali metal salts such as lithium salts, sodium salts orpotassium salts, alkaline-earth metal salts such as calcium salts, saltswith organic bases such as tromethamine, trimethylamine, triethylamine,2-aminobutane, tert-butylamine, diisopropylethylamine,n-butylmethylamine, cyclohexylamine, dicyclohexylamine,N-isopropylcyclohexylamine, furfurylamine, benzylamine,methylbenzylamine, dibenzylamine, N,N-dimethylbenzylamine,2-chlorobenzylamine, 4-methoxybenzylamine, 1-naphthylene methylamine,diphenylbenzylamine, triphenylamine, 1-naphthylamine,1-aminoanthorathene, 2-aminoanthorathene, dehydroabiethylamine,N-methylmorpholine, pyridine), basic amino acid salts such as argininesalts or lysine salts.

A solvate means a solvate with an organic solvent, a hydrate and thelike of the compound of the formula (I), its prodrug or itspharmaceutically acceptable salt, for example, monohydrate, dihydrate orthe like.

General processes for the preparation of the compounds of the formula(I) are illustrated as follows.

-   -   A is alkylene optionally intervened with a heteroatom,        optionally having an oxo group, optionally substituted with        halogen and/or optionally having an unsaturated bond;    -   R is —C(═O)—R¹, —CH₂—R¹, or tetrazolyl;    -   R¹ is hydroxy, alkyloxy, or optionally substituted amino;    -   m is 0 or 1;    -   provided that when m is 1, A is —CH═CH—CH₂—CH₂—CH₂— and        furthermore R is —C(═O)—R¹ wherein R¹ is hydroxy or alkyloxy,        and provided that when A is —CH₂—CH═CH—CH₂—CH₂—CH₂— and R is        —C(═O)—R¹ wherein R¹ is hydroxy or alkyloxy, a compound is        excluded;    -   p is 0 or 1, provided that when p=0, X¹ is not bonded to X³ via        X⁴;    -   X¹ and X³ are each independently optionally substituted aryl,        optionally substituted heteroaryl, or optionally substituted        non-aromatic heterocyclyl;    -   X² is a bond, —CH₂—, —CH₂—CH₂—, —C(═O)—, —O—, —S—, —SO—, —SO₂—,        —NH—, —N(CH₃)—, —C(═N—O—CH₃)—, —N═N—, —CH═CH—, —(C═O)—NH—,        —NH—(C═O)—, —CH₂—NH—, —NH—CH₂—, —CH₂—O—, —O—CH₂—, —CH₂—S—,        —S—CH₂—, —CH₂—SO₂—, —SO₂—CH₂—, —SO₂—NH—, —NH—SO₂—, —C(═CH₂)—,        —SO₂N(Me)—, —CH₂NHSO₂—, —CH₂NH—(C═O)—, —NH—C(═O)—NH, or        —NH—C(═O)—N(Me)—;    -   X⁴ is —C₂—, —CH₂—CH₂—, —C(═O)—, —SO—, —SO₂—, —(C═O)—NH—,        —NH—(C═O)—, —CH₂—NH—, —NH—CH₂—, —CH₂—O—, —O—CH₂—, —CH₂—S—,        —S—CH₂—, —CH₂—SO₂—, —SO₂—CH₂—, —SO₂—NH— or —NH—SO₂—.

As shown in the above process, the compound of the formula (I) can beprepared by reacting a carboxylic acid of the formula (M-2) or itsreactive derivative with an amino compound of the formula (M-1).

The reactive derivatives of carboxylic acid of the formula (M-2) meanthe corresponding acid halides (e.g., chloride, bromide, iodide),anhydrides (e.g., mixed anhydride with formic acid or acetic acid),active esters (e.g., N-hydroxysuccinimide ester), and the like, andinclude acylating agents used for the usual acylation of amino group.

For example, an acid halide is obtained by reacting the compound (M-2)with a thionyl halide (e.g., thionyl chloride), phosphorous halide(e.g., phosphorous trichloride, phosphorous pentachloride), oxalylhalide (e.g., oxalyl chloride), and the like, in accordance with knownmethods as described in the literatures.

The reaction can be conducted under a condition generally used for theacylation of amino group. For example, in the case of condensation withthe acid halide, the reaction is carried out in a solvent such as anether solvent (e.g., diethyl ether, tetrahydrofuran, dioxane), benzenesolvent (e.g., benzene, toluene, xylene), halogenated hydrocarbonsolvent (e.g., dichloromethane, dichloroethane, chloroform) as well asethyl acetate, dimethylformamide, dimethyl sulfoxide, acetonitrile, orthe like, if necessary, in the presence of a base (e.g., organic basesuch as triethylamine, pyridine, N,N-dimethylaminopyridine,N-methylmorpholine; inorganic base such as sodium hydroxide, potassiumhydroxide, potassium carbonate, or the like) under cooling, at roomtemperature, or under heating, preferably at a temperature ranging from−20° C. to ice-cooling temperature, or from room temperature to arefluxing temperature of the reaction system, during several min toseveral hr, preferably for 0.5 hr to 24 hr, more preferably for 1 hr to12 hr.

Unless R of a compound represented by the formula (M-1) is a carboxylgroup, a free form may be used without converting the carboxy group(M-2) into the reactive derivatives and the reaction may be conducted inthe presence of a condensing agent (e.g., dicyclohexylcarbodiimide(DCC), 1-ethyl-3-(3-methylaminopropyl)carbodiimide,N,N′-carbonyldiimidazole, or the like) usually used in the condensationreaction of amine and carboxylic acid.

When “optionally substituted aryl”, “optionally substituted heteroaryl”or “optionally substituted non-aromatic heterocyclyl” in X¹ or X³ of thecompound of the formula (M-2) is substituted with a hydroxy group or anamino group, such a compound can be used after protection by acetylgroup or the like in accordance with the well known method.

In the reaction of the other reactive derivatives or free acid (M-2)with the amine (M-1), the reaction conditions are determined accordingto the property of each reactive derivative or free acid, in accordancewith a known method. The reaction product can be purified in accordancewith a conventional purification, such as the extraction with a solvent,chromatography, recrystallization, and the like.

In an object compound of the present invention, various derivatives inwhich R is —C(═O)—R¹, —CH₂—R¹ or tetrazolyl (R¹ is hydroxy, alkyloxy oroptionally substituted amino) can be converted from a compound in whichR is carboxylic acid. For instance, a derivative of the ester or theamide can be prepared by esterification or amidation, in accordance withthe well known method. Furthermore, the ester derivative can beconverted by reduction to an alcoholic derivative, which can be derivedto an ether derivative by O-alkylation. A compound in which R is5-tetrazolyl, can be prepared by converting an amide derivative havingR; CONH₂ to R: CN by dehydration in accordance with the well knownmethod, followed by a reaction with sodium azide (J. Am. Chem. Soc.1958, 80, 3908) or trimethylsilylazide (J. Org. Chem. 1993, 58, 4139).

In this process, the starting compound (M-1) wherein R¹ is—CH₂—CH═CH—CH₂—CH₂—CH₂—COOMe, m is 0, Y is [2.2.1]bicyclic skeleton,7-(3-amino-bicyclo[2.2.1]hept-2-yl)-5-heptenoic acid methyl ester isdescribed in the Japanese Patent Publication (Kokoku) No. 79060/1993.The other starting compounds can be prepared from the aldehydederivative (Q is a protecting group such as benzyloxycarbonyl,t-butoxycarbonyl and the like) represented by a general formula (M-1a)or (M-1b) by one or more reaction(s) of a yilide compound under a Wittigreaction condition (Org. Reaction, 1965, 14, 270) in combination withother reactions. In a starting compound, various derivatives wherein Ris —C(═O)—R¹, —CH₂—R¹ or tetrazolyl (R¹ is hydroxy, alkyloxy oroptionally substituted amino) can be converted from a compound wherein Ris COOH.

For example, the aldehyde (M-1a) is reacted with(3-carboxypropyl)triphenylphosphonium salt under a well known Wittigreaction condition to give a starting material (M-5D), wherein A is—CH₂═CH—CH₂—CH₂—. The compound M-5D is hydrogenated in the presence ofpalladium, platinum and the like to give a starting material (M-5A),wherein A is —CH₂—CH₂—CH₂—CH₂—. Furthermore, after a Wittig reactionusing methoxymethyltriphenyl-phosphonium salt, followed by a hydrolysiswith hydrochloric acid, formic acid, acetic acid and the like canfurnish an aldehyde (M-1b) with one additional carbon atom and moreovera Wittig reaction with 2-(1,3-dioxoran-2-yl)ethyltriphenylphosphoniumsalt can give a compound represented by a general formula (M-1c). AJones oxidation (J. Chem. Soc., 1946, 39) of the compound gives astarting material (M-5B) wherein A is —CH₂—CH═CHCH₂— in the formula(M-1). And by the above similar method, after an aldehyde (M-1d) wasobtained by hydrogenation, followed by hydrolysis of the acetal withacid, either a Wittig reaction with a stable yield such as methyl(triphenylphophoranidene)acetate and the like or a Honer-Emmons reactionwith methyl dimethylphosphonoacetate can convert to a starting material(M-7I), wherein A is —CH₂—CH₂—CH₂—CH₂—CH═CH—. When the above mentionedreaction is applied to an aldehyde (M-1b), a corresponding startingmaterial (M-4B), wherein A is —CH₂CH═CH— is obtained and furthermore acorresponding starting material (M-4A) wherein A is —CH₂—CH₂—CH₂— isobtained by a hydrogenation of the double bond. When a starting materialwherein A is —CH₂—CH₂—CH₂—CH₂—O—CH₂— is required, a compound of theformula (M-4A) wherein R is CH₂OH can be reacted with halogenated aceticacid or its ester, ether, or amide and the like in the presence of abase in accordance with known methods as described in the literatures.

Amidation with a starting carboxylic acid (M-2) can be accomplishedafter a deprotection of an amino protecting group Q in a way ofconversion to α-chain, if necessary.

When p is 0, the carboxylic acid of the formula (M-2) can be prepared byreacting a carboxylic acid having X¹ or its reactive derivative with acompound having X³. A person ordinary skilled in the art can carry outsuch a reaction by selecting the kinds of reactions and their conditionsdepending on the kind of X².

A compound represented by the formula: X³—X²—X¹—COOH wherein X³ ispyrrolyl optionally substituted with alkyl, alkyloxy or halogen, indolyloptionally substituted with alkyl, alkyloxy or halogen, indolinyloptionally substituted with alkyl, alkyloxy or halogen or1,2,3,4-tetrahydroquinolyl optionally substituted with alkyl, alkyloxyor halogen; X² is —SO₂—, —S— or —CH₂—; X¹ is thienyl, or thepharmaceutically acceptable salt, or especially a substituentrepresented by the formula: X¹—X²—X³ is5-[(1-pyrrolyl)sulfonyl]thiophen-2-yl,5-[(2-methyl-1-pyrrolyl)sulfonyl]thiophen-2-yl or5-[(2,5-dimethyl-1-pyrrolyl)sulfonyl]thiophen-2-yl, or thepharmaceutically acceptable salt is important as an intermediate. Saltrefers to lithium salt, sodium salt, potassium salt, calcium salt,triethylammonium salt, pyridinium salt or the like.

When p is 0, a group of the formula: —NHCO—X¹—X²—X³ of the compound (I)can be introduced by reacting a carboxylic acid of the formula:X³—X²—X¹—COOH (M-2) or its reactive derivative with amine (M-1), or byreacting a carboxylic acid having X¹ or its reactive derivatives withamine (M-1) and reacting the obtained compound with a compound havingX³.

In case of the introduction of a substituent(s) into the “optionallysubstituted aryl”, “optionally substituted heteroaryl” or “optionallysubstituted non-aromatic heterocyclyl”, the change of the functionalgroup can be performed before or after reacting a carboxylic acid or itsreactive derivative thereof (M-2) with the amine (M-1).

In an aromatic part such as aryl, heteroaryl and the like, usual methodsof introduction or conversion of the functional group known for anaromatic ring can be applied. For example, the compound having anaromatic heterocycle substituted with a nitro group can be preparedthrough the nitration of the compound with a nitrating acid. Moreover,the compound having an aromatic heterocycle substituted with an aminogroup can be prepared through the reduction of the above-obtainedcompound with tin in the presence of hydrochloride. Moreover, thecompound having an aromatic heterocycle substituted with hydroxy groupcan be prepared through the diazonization of the above-obtained compoundand the hydrolysis with alkali. On the other hand, the compound havingan aromatic heterocycle substituted with an alkoxy group can be preparedthrough the reaction of the diazonium derivative with alcohol. Thecompound having an aromatic heterocycle substituted with halogen can beprepared through Sandmeyer reaction, the reaction of the diazoniumderivative with a copper salt (e.g., CuCl₂, CuBr₂). The compound havingan aromatic heterocycle substituted with halogen can be also preparedthrough the direct reaction of the compound having an aromaticheterocycle with chlorine and the like. Using the above-mentionedmethods appropriately, halogen can be introduced into a desiredposition(s). The group of alkyl, alkenyl or acyl group can be directlyintroduced into an aromatic heterocycle through Friedel Crafts reactionwith alkylating agent, an alkenylating agent, or an acylating agent,respectively, in the presence of anhydrous aluminum chloride and thelike.

The objective compound (I) of the present invention can be convertedinto a corresponding ester derivative, if desired. For example, theester derivative can be prepared by esterification of a carboxylic acidin accordance with a known method.

When using the compound (I) of the present invention in treatment, itcan be formulated into ordinary formulations for oral and parenteraladministration. A pharmaceutical composition containing the compound (I)of the present invention can be in the form for oral and parenteraladministration. Specifically, it can be formulated into formulations fororal administration such as tablets, capsules, granules, powders, syrup,and the like; or those for parenteral administration such as injectablesolution or suspension for intravenous, intramuscular, or subcutaneousinjection, inhalant, eye drops, nasal drops, suppositories, orpercutaneous formulations such as ointment.

In preparing the formulations, carriers, excipients, solvents, and basesknown to one having ordinary skill in the art may be used. In case oftablets, they are prepared by compressing or formulating an activeingredient together with auxiliary components. Examples of usableauxiliary components include pharmaceutically acceptable excipients suchas binders (e.g., cornstarch), fillers (e.g., lactose, microcrystallinecellulose), disintegrants (e.g., starch sodium glycolate) or lubricants(e.g., magnesium stearate). Tablets may be coated appropriately. In caseof liquid formulations such as syrups, solutions, or suspensions, theymay contain suspending agents (e.g., methyl cellulose), emulsifiers(e.g., lecithin), preservatives, and the like. In case of injectableformulations, it may be in the form of solution, suspension, or oily oraqueous emulsion, which may contain suspension-stabilizing agents ordispersing agent, and the like. In case of an inhalant, it is formulatedinto a liquid formulation applicable to an inhaler. In case of eyedrops, it is formulated into a solution or a suspension.

Especially, in case of a nasal drug for treating nasal blockage, it canbe used as a solution or suspension prepared by a conventionalformulating method, or administered as a powder formulated using apowdering agent (e.g., hydroxypropyl cellulose, carbopole) into thenasal cavity. Alternatively, it can be used as an aerosol filled into aspecial container together with a solvent of low boiling point.

In a case using as an eyewash drug for treating allergic conjunctivitis,it can be used as a solution or suspension of the compound or can beused by solving or suspending the compound before use. A stabilizingagent, solubilizing agent, suspending agent, emulsifier, buffer,preservatives and the like can be included. In a case using as aneyewash drug, aseptic treatment is preferable.

Pharmaceutical preparation of injection, oral agent, inhalation and thelike is preferable for treating asthma.

Although an appropriate dosage of the compound (I) varies depending onthe administration route, age, body weight, sex, or conditions of thepatient, and the kind of drug(s) used together, if any, and should bedetermined by the physician in the end, in the case of oraladministration, the daily dosage can generally be between 0.01–100 mg,preferably 0.01–10 mg, more preferably 0.01–1 mg, per kg body weight. Incase of parenteral administration, the daily dosage can generally bebetween 0.001–100 mg, preferably 0.001–1 mg, more preferably 0.001–0.1mg, per kg body weight. The daily dosage can be administered in 1–4divisions.

EXAMPLE

The following examples are provided to further illustrate the presentinvention and are not to be construed as limiting the scope.

Example 1

Preparation of (I-5A-59a), (I-5A-59b)

Potassium t-butoxide (4.32 g, 38.5 mmol) was added to a suspension of(3-carboxypropyl)triphenylphosphonium bromide (9.42 g, 22.0 mmol) in THF(45 ml) with cooling in ice. The mixture was stirred for 1 h and cooledto −10° C. A solution of compound (I) (3.0 g, 11.0 mmol) in THF (15 ml)was added dropwise over 15 min. The mixture was stirred at thetemperature for 1 h, diluted with water, washed twice with toluene,acidified (pH=1) with hydrochloric acid and extracted with ethylacetate. The extracts were washed with water and brine, dried andconcentrated. An excess diazomethane solution in ether was added to asolution of the residue in ethyl acetate (20 ml) with cooling in ice.The mixture was concentrated and purified by silica gel chromatography(hexane-ethyl acetate, 85:15) to give a compound (2) (3.32 g; yield85%).

Process 2

10% Palladium-carbon (0.32 g) was added to a solution of compound (2)(3.22 g, 9.0 mmol) in methanol (30 ml). The mixture was stirred under ahydrogen atmosphere for 17 h, filtered and concentrated to give acompound (3) (2.05 g; yield 100%)

Process 3

5-(2-Thienylthio)thiophene-2-carboxylic acid (233 mg, 0.96 mmol) and1-hydroxybenzotriazole (10.8 mg, 0.08 mmol) were added to a solution ofcompound (3) (180 mg, 0.80 mmol) in THF (8 ml) and1-ethyl-3-(3-dimethylaminopropyl)-carbodiimide (149 mg, 0.96 mmol) undercooling in ice. The mixture was stirred at room temperature for 14 h,diluted with ethyl acetate, washed with dilute hydrochloric acid, aq.sodium hydrogencarbonate successively, dried and concentrated. Theresidue was purified by silica gel chromatography (hexane-ethyl acetate,5:1) to give a compound (I-5A-59b) (325 mg; yield 90%).

Process 4

1N aq. lithium hydroxide (1.8 ml, 1.8 mmol) was added to a solution ofcompound (I-5A-59b) (325 mg, 0.72 mmol) in THF (8 ml). The mixture wasstirred at room temperature for 14 h, acidified and extracted with ethylacetate. The extracts were washed with water and brine, successively,dried and concentrated to give a compound (I-5A-59a) (300 mg; yield96%).

Example 2

Preparation of Compound (I-7M-1a), (I-7N-1a), (I-7N-1b)

Methyl bis(2,2,2-trifluoroethyl)phosphonoacetate (2.94 ml, 13.92 mmol)and 18-crown-6 (5.52 g, 20.88 mmol) in THF (100 ml) were cooled at −60°C. A solution of potassium bis(trimethylsilyl)amide (0.5 M toluenesolution, 27.8 ml, 13.9 mmol) was added. The mixture was stirred for 15h. A solution of compound (4) (2.0 g, 6.96 mmol) in THF (20 ml) wasadded dropwise during 15 min. The mixture was stirred at the sametemperature for 2 h. The temperature was raised to 0° C. and the mixturewas diluted with water and extracted with ethyl acetate. The extractswere washed with water and brine, successively, dried, concentrated andpurified by silica gel chromatography (hexane-ethyl acetaqte, 5:1) togive a compound (5) (2.10 g; yield 88%).

Process 2

Diisopropylaluminum hydride (1M toluene solution, 13.1 ml, 13.1 mmol)was added dropwise to a solution of compound (5) (1.80 g, 5.24 mmol) indichloromethane (20 ml)-hexane (20 ml) at −78° C. The mixture wasstirred at the temperature for 1 h. Methanol (1 ml) was added. Themixture was warmed to the room temperature. 2N Hydrochloric acid wasadded. The mixture was extracted with ethyl acetate. The extracts werewashed with sodium hydrogencarbonate and brine successively, dried,concentrated and purified by silica gel chromatography (hexane-ethylacetate, 7:3) to give a compound (6) (5.92 g; yield 96%).

Process 3

A mixture of compound (6) (1.58 g, 5.01 mmol), t-butyl bromoacetate(1.05 ml, 6.50 mmol), tetrabutylammonium hydrogensulfate (170 mg, 0.5mmol) and 50% sodium hydroxide (4 ml) were vigorously stirred at roomtemperature for 18 h. The phase of toluene was separated, washed withwater and brine successively, dried and concentrated. The residueobtained, trifluoroacetic acid (6.38 ml, 83 mmol) and anisole (3.37 ml.31 mmol) were stirred at 60° C. for 15 h and concentrated under areduced pressure. The residue was washed with hexane. Methanol (20 ml)and conc. sulfuric acid (0.44 ml) were added. The mixture was heatedunder reflux for 2 h. 2N sodium hydroxide was added to be alkaline. Themixture was extracted with ethyl acetate. The extracts were washed withwater and brine successively, dried and concentrate to give a compound(7) (461 mg; yield 44%).

Process 4

5-(2-Methyl-1-pyrrolylsulfonyl)thiophene-2-carboxylic acid (21.8 mg,0.85 mmol) and 1-hydroxybenzotriazole (13 mg, 0.09 mmol) were added to asolution of compound (7) (215 mg, 0.85 mmol) in THF (6 ml).1-Ethyl-3-(3-dimethylaminopropyl)-carbodiimide (137 mg, 1.02 mmol) wasfurther added under cooling in ice. The mixture was stirred at roomtemperature for 16 h, diluted with ethyl acetate, washed with dilutehydrochloric acid and sodium hydrogencarbonate successively, dried andconcentrated. The residue was purified by silica gel chromatography(hexane-ethyl acetate 2:1) to give a compound (I-7N-1b) (328 mg; yield78%).

Process 5

1 N Sodium hydroxide solution (1.57 ml, 1.57 mmol) was added to asolution of compound (I-7N-1b) (310 mg, 0.63 mmol) in THF (3.2ml)-methanol (6.3 ml) and the mixture was stirred at room temperature 16h. 2N Hydrochloric acid was added to acidify and the mixture wasextracted with ethyl acetate. The extracts were washed with water andbrine successively, dried and concentrated to give a compound (I-7N-1a)(399 mg; yield 73%).

Process 6

10% Palladium-carbon (170 mg, 0.36 mmol) was added to a solution ofcompound (1-7N-1a) (170 mg, 0.36 mmol) in methanol (5 ml). The mixturewas stirred under a hydrogen atmosphere for 17 h and filtered. Thefiltrate was concentrated to give a compound (I-7M-1a) (162 mg; yield95%).

Example 3 Preparation of Compounds (I-7I-55a), (II-7I-55b)

Potassium t-butoxide (6.73 g, 60.0 mmol) was added to a suspension of2-(1,3-dioxolan-2-yl)ethyltriphenylphosphonium bromide (13.28 g, 30.0mmol) in THF (60 ml) at −30° C. The mixture was stirred at −30° C. to 0°C. for 1 h. A solution of compound (8) (5.62 g, 20.0 mmol) in THF (40ml) was added dropwise at −25° C. during 15 min. The mixture was warmedto 0° C., stirred for 1.5 h, diluted with water and extracted with ethylacetate. The extracts were washed with water and brine, dried andconcentrated. The residue was purified by silica gel chromatography(hexane-ethyl acetate 85:15) to give a compound (9) (6.27 g, yield 86%)

Process 2

10% Palladium-carbon (0.21 g) was added to a solution of compound (9)(4.10 g, 11.2 mmol) in methanol (41 ml). The mixture was stirred under ahydrogen atmosphere for 2 h and filtered. The filtrate was concentratedto give a residue. Pydidinium p-toluenesulfonate (503 mg, 2.0 mmol) wasadded to a solution of the residue in acetone-water (4:1, 50 ml). Themixture was heated under reflux for 16 h, diluted with water andextracted with ethyl acetate. The extracts were washed with water andbrine, dried and concentrated. A mixture of the residue and methyl(triphenylphosphoraniliden)acetate (2.93 g, 8.76 mmol) in toluene (35ml) was stirred at room temperature for 18 h, diluted with ethylacetate, washed with water and brine and concentrated. The residue waspurified by silica gel chromatography in (hexane-ethyl acetate 35:15) togive a compound (10) (2.71 g; yield 71%).

Process 3

Trifluoroacetic acid (3.82 ml, 49.5 mmol) was added to a solution ofcompound (10) (2.35 g, 6.19 mmol) in dicholoromethane (38 ml) and themixture was stirred at room temperature for 3 h and concentrated under areduced pressure. The residue was dissolved in toluene (50 ml) and water(10 ml). 2N Sodium hydroxide was added to be alkaline in the aq. layer.The toluene phase was separated, washed with water and brine, dried andconcentrated to give a compound (11) (1.70 g; yield 98%).

Process 4

1-Ethyl-3-(3-dimethylaminopropyl)-carbodiimide (252 mg, 1.62 mmol) wasadded to a mixture of a compound (11) (433 mg, 1.55 mmol),5-(2-methyl-1-pyrrolylsulfonyl)thiophen-2-carboxylic acid (400 mg, 1.47mmol) and 1-hydroxybenzotriazole (20 mg, 0.15 mmol) in THF (6 ml) withcooling in ice. The mixture was stirred at room temperature for 16 h,diluted with ethyl acetate, washed with dilute hydrochloric acid and aq.sodium hydrogencarbonate successively, dried and concentrated. Theresidue was purified by silica gel chromatography (hexane-ethyl acetate,4:1) to give a product (II-7I-55b) (585 mg; yield 74%).

Process 5

2N Lithium hydroxide (1.58 ml, 3.15 mmol) was added to a solution ofcompound (II-7I-55b) (560 mg, 1.05 mmol) in THF (8 ml). A mixture wasstirred at room temperature for 48 h, acidified with 2N Hydrochloricacid and extracted with ethyl acetate. The extracts were washed withwater and brine successively, dried and concentrated. The residue waspurified by silica gel chromatography (hexane-ethyl acetate, 1:3) togive a compound (II-7I-55a) (399 mg; yield 73%).

Example 4

Preparation of Compounds (I-7A-1e), (I-7E-1e)

Oxalyl chloride (0.236 ml, 2.71 mmol) and N,N-dimethylformamide (a drop)were added to a solution compound (12) (840 mg, 2.26 mmol) indichloromethane (20 ml) with cooling in ice. The mixture was stirred for30 min and concentrated under a reduced pressure. The residue wasdissolved in dichloromethane (20 ml). Methanesulfonamide (258 mg, 2.71mmol) and 1,8-diazabicyclo[5.4.0]-7-undecene (0.744 ml, 4.97 mmol) wereadded. The mixture was stirred for 2.5 h, diluted with ethyl acetate,washed with dilute hydrochloric acid, aq. sodium hydrogencarbonate andbrine successively, dried and concentrated. Trifluoroacetic acid (25 ml)and anisole (2 ml, 18.40 mmol) were added to the residue. The mixturewas stirred at 50° C. for 13 h and concentrated under a reducedpressure. The oily residue was washed with hexane to give a compound(13) (0.776 g; yield 65%).

Process 2

Oxalyl chloride (0.081 ml, 0.929 mmol) and N,N-dimethylformamide (adrop) were added to a solution5-(1-pyrrolylsulfonyl)thiophene-2-carboxylic acid (209 mg, 0.812 mmol)in dichloromethane (4 ml) with cooling in ice. The mixture was stirredfor 20 min and at room temperature for 40 min and concentrated under areduced pressure. The residue was dissolved in dichloromethane (4 ml). Asolution of compound (13) (0.42, 0.774 mmol) in dichloromethane (4ml)-THF (3 ml) and triethylamine (0.486 ml, 3.49 mmol) were added to thesolution with cooling in ice. The mixture was stirred for 1.5 h and atroom temperature for 19 h, diluted with ethyl acetate, washed withdilute hydrochloric acid, aq. sodium hydrogencarbonate and brinesuccessively, dried and concentrated. The residue was purified by silicagel chromatography (hexane-ethyl acetate-acetic acid, 1:1:0.003) to givea compound (I-7E-1e) (157 mg; yield 37%).

Process 3

20% Palladium hydroxide-carbon (64 mg) was added to a solution ofcompound (I-7E-1e) (116 mg, 0.21 mmol) in methanol (3 ml). The mixturewas stirred under a hydrogen atmosphere for 20 h and filtered. Thefiltrate was concentrated to give a compound (I-7A-1e) (109 mg; yield94%).

Example 5

Preparation of Compound (Formula: X³—X²—X¹—COOH)

5-Bromothiophene-2-sulfonyl chloride was reacted directly with a pyrrolederivative or the acid chloride was converted to the sulfonamidefollowed by condensation with 2,5-dimethoxytetrahydro-derivative to givea sulfonylpyrrole derivative. Then, the product was converted to theorganolithium or the organomagnesium compound by a halogen-metalexchange reaction, followed by reacting with carbon dioxide to give adesired compound.

5-(1-Pyrrolylsulfonyl)-2-thiophenecarboxylic acid

mp 191–194° C.; ¹H-NMR (CDCl₃) δ6.36 (2H, t, J=2.4 Hz), 7.18 (2H, t,J=2.4 Hz), 7.61 (1H, d, J=4.2 Hz), 7.74 (1H, d, J=4.2 Hz).

5-(2-Methyl-1-pyrrolylsulfonyl)-2-thiophenecarboxylic acid

mp 159–160° C.; ¹H-NMR (CDCl₃) δ2.40 (3H, d, J=0.9 Hz), 6.01 (1H, m),6.23 (1H, t, J=3.0 Hz), 7.20 (1H, dd, J=1.8, 3.6 Hz), 7.58 (1H, d, J=4.2Hz), 7.76 (1H, d, J=4.2 Hz).

5-(2,5-Dimethyl-1-pyrrolylsulfonyl)-2-thiophenecarboxylic acid

mp 167–171° C.; ¹H-NMR (CDCl₃) δ2.43 (6H, s), 5.90 (2H, s), 7.52 (1H, d,J=3.9 Hz), 7.75 (1H, d, J=3.9 Hz).

The structure and physical property of the compound prepared inaccordance with the above examples are shown below. Each sign used for—X¹—X²—X³ and A in Tables means the sign represented before.

TABLE 1

Compd. No.. —X¹—X²—X³ A R I-4A-1a 1 4A CO₂H I-4B-1a 1 4B CO₂H I-4C-1a 14C CO₂H I-4D-1a 1 4D CO₂H I-4E-1a 1 4E CO₂H I-4F-1a 1 4F CO₂H I-5A-1a 15A CO₂H I-5A-1b 1 5A CO₂Me I-5A-31a 31 5A CO₂H I-5A-47a 47 5A CO₂HI-5A-55a 55 5A CO₂H I-5A-59a 59 5A CO₂H I-5A-59b 59 5A CO₂Me I-5A-80a 805A CO₂H I-5A-88a 88 5A CO₂H I-5A-88b 88 5A CO₂Me I-5A-104a 104 5A CO₂HI-5A-126a 126 5A CO₂H I-5A-143a 143 5A CO₂H I-5A-197a 197 5A CO₂HI-5B-1a 1 5B CO₂H I-5B-47a 47 5B CO₂H I-5B-59a 59 5B CO₂H I-5C-1a 1 5CCO₂H I-5C-1b 1 5C CO₂Me I-5C-55a 55 5C CO₂H I-5C-31a 31 5C CO₂H I-5C-47a47 5C CO₂H I-5C-88a 88 5C CO₂H I-5D-1a 1 5D CO₂H I-5E-1a 1 5E CO₂HI-5E-55a 55 5E CO₂H I-5F-1a 1 5F CO₂H I-5F-47a 47 5F CO₂H I-5G-47a 47 5GCO₂H I-6A-1a 1 6A CO₂H I-6A-31a 31 6A CO₂H I-6A-55a 55 6A CO₂H I-6A-88a88 6A CO₂H I-6B-1a 1 6B CO₂H I-6B-31a 31 6B CO₂H I-6B-88a 88 6B CO₂HI-6C-1a 1 6C CO₂H

TABLE 2

Compd. No.. —X¹—X²—X³ A R I-6D-1a 1 6D CO₂H I-6E-1a 1 6E CO₂H I-6E-59a59 6E CO₂H I-6F-1a 1 6E CO₂H I-6G-1a 1 6G CO₂H I-7A-1a 1 7A CO₂H I-7A-1b1 7A CO₂Me I-7A-1c 1 7A CONH₂ I-7A-1e 1 7A CONHSO₂Me I-7A-1h 1 7A CH₂OHI-7A-1i 1 7A CH₂OMe I-7A-31a 31 7A CO₂H I-7A-47a 47 7A CO₂H I-7A-47i 477A CH₂OMe I-7A-55a 55 7A CO₂H I-7A-59a 59 7A CO₂H I-7A-80a 80 7A CO₂HI-7A-88a 88 7A CO₂H I-7A-88e 88 7A CONHSO₂Me I-7A-88h 88 7A CH₂OHI-7A-88i 88 7A CH₂OMe I-7A-104a 104 7A CO₂H I-7A-143a 143 7A CO₂HI-7A-197a 197 7A CO₂H I-7A-315a 315 7A CO₂H I-7A-316a 316 7A CO₂HI-7B-1a 1 7B CO₂H I-7C-1a 1 7C CO₂H I-7D-1a 1 7D CO₂H I-7E-1c 1 7E CONH₂I-71-1d 1 7E CONHMe I-71-1e 1 7E CONHSO₂Me I-71-1f 1 7E CON(Me)SO₂MeI-7E-1g 1 7E 5-tetrazolyl I-7E-1h 1 7E CH₂OH I-71-1i 1 7E CH₂OMeI-71-47c 47 7E CONH₂ I-71-47i 47 7E CH₂OMe I-7E-88e 88 7E CONHSO₂MeI-7E-88h 88 7E CH₂OH I-71-88i 88 71 CH₂OMe I-7F-1a 1 7F CO₂H

TABLE 3

Compd. No.. —X¹—X²—X³ A R I-7F-31a 31 7F CO₂H I-7F-47a 47 7F CO₂HI-7F-88a 88 7F CO₂H I-7F-143a 143 7F CO₂H I-7G-1a 1 7G CO₂H I-7G-88a 887G CO₂H I-7G-126a 126 7G CO₂H I-7I-1a 1 7H CO₂H I-7I-1a 1 7I CO₂HI-7I-1b 1 7I CO₂Me I-7I-1c 1 7I CONH₂ I-7I-1e 1 7I CONHSO₂Me I-7I-31a 317I CO₂H I-7I-47a 47 7I CO₂H I-7I-55a 55 7I CO₂H I-7I-59a 59 7I CO₂HI-7I-80a 80 7I CO₂H I-7I-88a 88 7I CO₂H I-7I-93a 93 7I CO₂H I-7I-126a126 7I CO₂H I-7I-143a 143 7I CO₂H I-7I-197a 197 7I CO₂H I-7I-270a 270 7ICO₂H I-7I-307a 307 7I CO₂H I-7I-327a 327 7I CO₂H I-7I-332a 332 7I CO₂HI-7I-343a 343 7I CO₂H I-7I-385a 385 7I CO₂H I-7I-389a 389 7I CO₂HI-7I-391a 391 7I CO₂H I-7J-1a 1 7J CO₂H I-7J-31a 31 7J CO₂H I-7K-1a 1 7KCO₂H I-7K-47a 47 7K CO₂H I-7K-59a 59 7K CO₂H I-7K-143a 143 7K CO₂HI-7L-1a 1 7L CO₂H I-7M-1a 1 7M CO₂H I-7M-1b 1 7M CO₂Me I-7M-1c 1 7MCONH₂ I-7M-1e 1 7M CONHSO₂Me I-7M-31a 31 7M CO₂H I-7M-40a 40 7M CO₂H

TABLE 4

Compd. No.. —X¹—X²—X³ A R I-7M-43a 43 7M CO₂H I-7M-47a 47 7M CO₂HI-7M-55a 55 7M CO₂H I-7M-59a 59 7M CO₂H I-7M-80a 80 7M CO₂H I-7M-88a 887M CO₂H I-7M-88e 88 7M CONHSO₂Me I-7M-88h 88 7M CH₂OH I-7M-88i 88 7MCH₂OMe I-7M-104a 104 7M CO₂H I-7M-126a 126 7M CO₂H I-7M-143a 143 7M CO₂HI-7M-197a 197 7M CO₂H I-7M-270a 270 7M CO₂H I-7M-307a 307 7M CO₂HI-7M-315a 315 7M CO₂H I-7M-316a 316 7M CO₂H I-7M-317a 317 7M CO₂HI-7M-318a 318 7M CO₂H I-7M-327a 327 7M CO₂H I-7M-329a 329 7M CO₂HI-7M-330a 330 7M CO₂H I-7M-331a 331 7M CO₂H I-7M-332a 332 7M CO₂HI-7M-333a 333 7M CO₂H I-7M-334a 334 7M CO₂H I-7M-336a 336 7M CO₂HI-7M-337a 337 7M CO₂H I-7M-342a 342 7M CO₂H I-7M-343a 343 7M CO₂HI-7M-385a 385 7M CO₂H I-7M-389a 389 7M CO₂H I-7M-390a 390 7M CO₂HI-7M-391a 391 7M CO₂H I-7M-392a 392 7M CO₂H I-7M-393a 393 7M CO₂HI-7M-396a 396 7M CO₂H I-7M-412a 412 7M CO₂H I-7M-424a 424 7M CO₂HI-7M-446a 446 7M CO₂H I-7M-447a 447 7M CO₂H I-7M-448a 448 7M CO₂HI-7N-1a 1 7N CO₂H

TABLE 5

Compd. No.. —X¹—X²—X³ A R I-7N-1b 1 7N CO₂Me I-7N-55a 55 7N CO₂HI-7N-88a 88 7N CO₂H I-7N-143a 143 7N CO₂H I-70-1a 1 7O CO₂H I-7P-1a 1 7PCO₂H I-7P-1e 1 7P CONHSO₂Me I-7Q-1a 1 7Q CO₂H I-7R-1a 1 7R CO₂H I-7R-59a59 7R CO₂H I-7R-88a 88 7R CO₂H I-7R-270a 270 7R CO₂H I-7R-307a 307 7RCO₂H I-7S-1a 1 7S CO₂H I-7T-1a 1 7T CO₂H I-8A-1a 1 8A CO₂H I-8A-47a 478A CO₂H I-8A-88a 88 8A CO₂H I-8B-1a 1 8B CO₂H I-8B-47a 47 8B CO₂HI-8B-88a 88 8B CO₂H I-8C-1a 1 8C CO₂H I-8C-88a 88 8C CO₂H I-9A-1a 1 9ACO₂H I-9A-47a 47 9A CO₂H I-9A-88a 88 9A CO₂H I-9B-1a 1 9B CO₂H I-9B-47a47 9B CO₂H I-9B-88a 88 9B CO₂H

TABLE 6

Compd. No.. —X¹—X²—X³ A R II-4A-55a 55 4A CO₂H II-4B-55a 55 4B CO₂HII-4C-55a 55 4C CO₂H II-4D-55a 55 4D CO₂H II-4E-55a 55 4E CO₂H II-4F-55a55 4F CO₂H II-5A-1a 1 5A CO₂H II-5A-1b 1 5A CO₂Me II-5A-31a 31 5A CO₂HII-5A-47a 47 5A CO₂H II-5A-55a 55 5A CO₂H II-5A-55c 55 5A CONH₂II-5A-55g 55 5A 5-tetrazolyl II-5A-59a 59 5A CO₂H II-5A-80a 80 5A CO₂HII-5A-88a 88 5A CO₂H II-5A-88b 88 5A CO₂Me II-5A-104a 104 5A CO₂HII-5A-126a 126 5A CO₂H II-5A-143a 143 5A CO₂H II-5A-197a 197 5A CO₂H

TABLE 7

Compd. No.. —X¹—X²—X³ A R Il-5B-1a 1 5B CO₂H II-5B-47a 47 5B CO₂HII-5B-55a 55 5B CO₂H II-5C-1a 1 5C CO₂H II-5C-1b 1 5C CO₂Me II-5C-55a 555C CO₂H II-5C-88a 88 5C CO₂H II-5D-1a 1 5D CO₂H II-5E-1a 1 5E CO₂HII-5E-55a 55 5E CO₂H II-5F-31a 31 5F CO₂H II-5F-47a 47 5F CO₂H II-5F-55a55 5F CO₂H II-5F-88a 88 5F CO₂H II-5G-47a 47 5G CO₂H Il-6A-1a 1 6A CO₂HII-6A-31a 31 6A CO₂H II-6A-55a 55 6A CO₂H II-6A-88a 88 6A CO₂H Il-6B-1a1 6B CO₂H II-6B-31a 31 6B CO₂H II-6B-55a 55 6B CO₂H II-6B-88a 88 6B CO₂H

TABLE 8

Compd. No.. —X¹—X²—X³ A R II-6C-31a 31 6C CO₂H Il-6D-1a 1 6D CO₂HII-6E-1a 1 6E CO₂H II-6E-59a 59 6E CO₂H II-6F-1a 1 6F CO₂H II-6G-1a 1 6GCO₂H II-7A-1a 1 7A CO₂H II-7A-1b 1 7A CO₂Me II-7A-1c 1 7A CONH₂II-7A-31a 31 7A CO₂H II-7A-47a 47 7A CO₂H II-7A-55a 55 7A CO₂H II-7A-55e55 7A CONHSO₂Me II-7A-55g 55 7A 5-tetrazolyl II-7A-59a 59 7A CO₂HII-7A-80a 80 7A CO₂H II-7A-88a 88 7A CO₂H II-7A-88e 88 7A CONHSO₂MeII-7A-88h 88 7A CH₂OH II-7A-88i 88 7A CH₂OMe II-7A-104a 104 7A CO₂HII-7A-143a 143 7A CO₂H II-7A-197a 197 7A CO₂H II-7A-315a 315 7A CO₂HII-7A-316a 316 7A CO₂H II-7B-55a 55 7B CO₂H II-7C-1a 1 7C CO₂H II-7D-1a1 7D CO₂H II-7E-1c 1 7E CONH₂ II-7E-1d 1 7E CONHMe II-7E-1e 1 7ECONHSO₂Me II-7E-1f 1 7E CON(Me)SO₂Me II-7E-1g 1 7E 5-tetrazolyl II-7E-1h1 7E CH₂OH II-7E-1i 1 7E CH₂OMe II-7E-47c 47 7E CONH₂ II-7E-55c 55 7ECONH₂ II-7E-55e 55 7E CONHSO₂Me II-7E-55g 55 7E 5-tetrazolyl II-7E-88e88 7E CONHSO₂Me II-7E-88h 88 7E CH₂OH II-7E-88i 88 7E CH₂OMe II-7F-1a 17F CO₂H

TABLE 9

Compd. No.. —X¹—X²—X³ A R II-7F-47a 47 7F CO₂H II-7F-55a 55 7F CO₂HII-7F-88a 88 7F CO₂H I1-7F-143a 143 7F CO₂H II-7G-1a 1 7G CO₂H II-7H-1a1 7H CO₂H II-7I-1a 1 7I CO₂H II-7I-1b 1 7I CO₂Me II-7I-1c 1 7I CONH₂II-7I-1e 1 7I CONHSO₂Me II-7I-31a 31 7I CO₂H I1-7I-47a 47 7I CO₂H1I-7I-55a 55 7I CO₂H II-7I-55b 55 7I CO₂Me II-7I-59a 59 7I CO₂HII-7I-80a 80 7I CO₂H II-7I-88a 88 7I CO₂H II-7I-104a 104 7I CO₂HII-7I-126a 126 7I CO₂H II-7I-197a 197 7I CO₂H II-7I-239a 239 7I CO₂HII-7I-270a 270 7I CO₂H II-7I-327a 327 7I CO₂H II-7I-332a 332 7I CO₂HII-7I-343a 343 7I CO₂H II-7I-389a 389 7I CO₂H II-7I-391a 391 7I CO₂HII-7J-1a 1 7I CO₂H II-7J-55a 55 7I CO₂H II-7K-1a 1 7K CO₂H II-7K-47a 477K CO₂H II-7K-55a 55 7K CO₂H II-7K-59a 59 7K CO₂H II-7K-143a 143 7K CO₂HII-7L-1a 1 7L CO₂H II-7L-55a 55 7L CO₂H II-7M-1a 1 7M CO₂H II-7M-1b 1 7MCO₂Me II-7M-1c 1 7M CONH₂ II-7M-1e 1 7M CONHSO₂Me II-7M-1k 1 7MCONHSO₂Ph II-7M-31a 31 7M CO₂H II-7M-40a 40 TM CO₂H

TABLE 10

Compd. No.. —X¹—X²—X³ A R II-7M-43a 43 7M CO₂H II-7M-47a 47 7M CO₂HII-7M-55a 55 7M CO₂H II-7M-59a 59 7M CO₂H II-7M-80a 80 7M CO₂H II-7M-88a88 7M CO₂H II-7M-88e 88 7M CONHSO₂Me II-7M-88h 88 7M CH₂OH II-7M-88i 887M CH₂OMe II-7M-104a 104 7M CO₂H II-7M-126a 126 7M CO₂H II-7M-143a 1437M CO₂H II-7M-197a 197 7M CO₂H II-7M-239a 239 7M CO₂H II-7M-270a 270 7MCO₂H II-7M-307a 307 7M CO₂H II-7M-327a 327 7M CO₂H II-7M-329a 329 7MCO₂H II-7M-330a 330 7M CO₂H II-7M-331a 331 7M CO₂H II-7M-332a 332 7MCO₂H II-7M-333a 333 7M CO₂H II-7M-334a 334 7M CO₂H II-7M-336a 336 7MCO₂H II-7M-343a 343 7M CO₂H II-7M-385a 385 7M CO₂H II-7M-389a 389 7MCO₂H II-7M-390a 390 7M CO₂H II-7M-391a 391 7M CO₂H II-7M-392a 392 7MCO₂H II-7M-393a 393 7M CO₂H II-7N-1a 1 7N CO₂FI II-7N-55a 55 7N CO₂HII-7N-88a 88 7N CO₂H II-7N-143a 143 7N CO₂H II-70-55a 55 7O CO₂HII-7P-55a 55 7P CO₂H II-7P-55e 55 7P CONHSO₂Me II-7P-55j 55 7PCONHSO₂CF₃ II-7Q-1a 1 7Q CO₂H II-7Q-55a 55 7Q CO₂H II-7R-55a 55 7R CO₂HII-7R-88a 88 7R CO₂H

TABLE 11

Compd. No.. —X¹—X²—X³ A R II-7R-270a 270 7R CO₂H II-7S-1a 1 7S CO₂HII-7S-47a 47 7S CO₂H II-7S-55a 55 7S CO₂H II-7T-55a 55 7T CO₂H II-7U-31a31 7U CO₂H II-7U-55a 55 7U CO₂H II-7U-88a 88 7U CO₂H II-7V-55a 55 7VCO₂H II-8A-1a 1 8A CO₂H II-8A-47a 47 8A CO₂H II-8A-88a 88 8A CO₂HII-8B-1a 1 8B CO₂H II-8B-47a 47 8B CO₂H II-8B-88a 88 8B CO₂H II-8C-55a55 8C CO₂H II-8C-88a 88 8C CO₂H II-9A-1a 1 9A CO₂H II-9A-47a 47 9A CO₂HII-9A-88a 88 9A CO₂H II-9B-1a 1 9B CO₂H II-9B-47a 47 9B CO₂H II-9B-88a88 9B CO₂H

TABLE 12

Compd. No.. —X¹—X²—X³ A R III-5A-1a 1 5A CO₂H III-5A-47a 47 5A CO₂HIII-5A-55a 55 5A CO₂H III-5A-80a 80 5A CO₂H III-7A-1a 1 7A CO₂HIII-7A-47a 47 7A CO₂H III-7A-55a 55 7A CO₂H III-7A-80a 80 7A CO₂H

TABLE 13

Compd. No.. —X¹—X²—X³ A R IV-5A-1a 1 5A CO₂H IV-5A-47a 47 5A CO₂HIV-7A-1a 1 7A CO₂H IV-7A-47a 47 7A CO₂H

TABLE 14

Compd. No.. —X¹—X²—X³ A R V-5A-88a 88 5A CO₂H V-7A-88a 88 7A CO₂H

TABLE 15

Compd. No.. —X¹—X²—X³ A R VI-6A-1a 1 6A CO₂H VI-6A-31a 31 6A CO₂HVI-6A-40a 40 6A CO₂H VI-6A-47a 47 6A CO₂H VI-6A-55a 55 6A CO₂H VI-6A-80a80 6A CO₂H VI-6A-88a 88 6A CO₂H VI-6A-104a 104 6A CO₂H VI-6A-122a 122 6ACO₂H VI-6A-123a 123 6A CO₂H VI-6A-124a 124 6A CO₂H VI-6A-133a 133 6ACO₂H

TABLE 16

Compd. No.. —X¹—X²—X³ A R VII-6A-1a 1 6A CO₂H VII-6A-47a 47 6A CO₂HVII-6A-88a 88 6A CO₂H

TABLE 17 Compd. No.. Physical property I-4B-1a ¹H-NMR(CD₃OD) δ1.24–2.33(11H, m), 2.46(1H, m), 3.69–3.76(2H, m), 6.11(1H, dt,J=7.8and33.3Hz), 6.36(2H, m), 7.23(2H, m), 7.71(2H, m), 8.54(1H, br);IR(CHCl₃)3442, 2877, 1741, 1657, 1529, 1504, 1456, 1383, 1167, 1076,1057, 1036cm⁻¹; [α]_(D) ²⁵+37.7±0.7° (c=1.05, MeOH) I-4E-1a¹H-NMR(CDCl₃) δ 1.26–1.76(7H, m), 2.10(1H, m), 2.47 (1H, m), 3.35(1H,dd, J=8.4and9.0Hz), 3.58(1H, dd, J= 6.3and8.4Hz), 3.98(1H, d, J=16.2Hz),4.08(1H, m), 4.13(1H, d, J=16.2Hz), 6.27(1H, d, J=8.1Hz), 6.34 (2H, d,J=4.8Hz), 7.15(2H, d, J=4.8Hz), 7.37(1H, d, J=4.2Hz), 7.58(1H, d,J=4.2Hz); IR(CHCl₃)3440, 2958, 2879, 1753, 1734, 1655, 1533, 1508, 1477,1456, 1427, 1383, 1315, 1167, 1122, 1057, 1034cm⁻¹; [α]_(D) ²⁴+41.7±0.8°(c=1.00, CHCl₃)Anal.(C₁₉H₂₂N₂O₆S₂·0.6H₂O) Calcd.(%): C, 50.79;H, 5.20; N, 6.23; S, 14.27Found(%): C, 50.76; H, 5.00; N, 6.26; S, 14.09I-4F-1a mp126–128°C.; ¹H-NMR(CD₃OD) δ 1.26–1.66(8H, m), 2.03(1H, m),2.48(1H, m), 2.57(1H, m), 3.76(1H, m), 5.69(1H, dt, J=8.1and21.3Hz),6.36(2H, m), 7.23 (2H, m), 7.72(2H, m), 8.53(1H, d, J=5.4Hz); IR(CHCl₃)3417, 3322, 2958, 2877, 1730, 1653, 1535, 1508, 1456, 1427, 1379,1302, 1167, 1128, 1057, 1036cm⁻¹; [α]_(D) ²⁵+68.3±1.0°(c=1.04,MeOH)Anal. (C₂₀H₂₁FN₂O₅S₂·0.9H₂O)Calcd.(%): C, 51.52; H, 4.90; N, 5.98;F, 4.05; S, 13.68Found(%): C, 51.46; H, 4.62; N, 5.72; F, 3.72; S, 12.93I-5A-1a ¹H-NMR(CDCl₃) δ 1.02(1H, m), 1.23–1.44(8H, m), 1.54–1.65(4H, m),2.00(1H, m), 2.29–2.36(2H, m), 2.49 (1H, brs), 3.80(1H, m), 6.17(1H, d,J=7.5Hz), 6.33–6.34 (2H, m), 7.15–7.16(2H, m), 7.35(1H, d, J=3.9Hz),7.55(1H, d, J=3.9Hz); IR(CHCl₃)3516, 3442, 1709, 1658, 1529, 1504, 1456,1383, 1192, 1167, 1057, 1034cm⁻¹; [α]_(D) ²⁷+48.7±0.9°(c=1.006,MeOH)Anal. (C₂₁H₂₆N₂O₅S₂)Calcd.(%): C, 55.98; H, 5.82; N, 6.22; S,14.23Found(%): C, 56.10; H, 5.81; N, 6.08; S, 13.77 I-5A-31a¹H-NMR(CDCl₃) δ 0.95(1H, m), 1.16–1.70(12H, m), 1.97 (1H, m), 2.32(2H,t, J=7.2Hz), 2.48(1H, m), 3.81(1H, m), 4.14(2H, s), 5.83(1H, d,J=6.6Hz), 6.77(1H, d, J= 3.3Hz), 7.21–7.37(6H, m); IR(CHCl₃)3514, 3446,3427, 1709, 1643, 1543, 1506, 1456cm⁻¹; [α]_(D) ^(24.0)+46.9±0.9°(c=1.011, MeOH)Anal.(C₂₄H₂₉NO₃S·0.5H₂O)Calcd.(%): C, 68.54; H, 7.19; N,3.33; S, 7.62Found(%): C, 68.62; H, 7.03; N, 3.47; S, 7.54

TABLE 18 Compd. No.. Physical property I-5A-47a ¹H-NMR(CDCl₃) δ 1.03(1H,m), 1.18–1.70(12H, m), 1.98 (1H, m), 2.32(2H, dt, J=8.1, 2.1Hz),2.50(1H, m), 3.81 (1H, m), 6.19(1H, d, J=7.8Hz), 7.11 (1H, dd, J=5.1,3.9Hz), 7.39(1H, d, J=3.9Hz), 7.61(1H, d, J=3.9Hz), 7.70(1H, dd, J=5.1,1.2Hz), 7.75(1H, dd, J=3.9, 1.2Hz); IR(CHCl₃)3512, 3442, 3375, 2679,1709, 1655, 1529, 1504, 1402, 1336, 1153, 1095, 1022cm⁻¹; [α]_(D)^(24.0+) 48.6±0.9°(c=1.009, MeOH)Anal. (C₂₁H₂₅NO₅S₃·0.2H₂O)Calcd.(%): C,53.53; H, 5.43; N, 2.97; S, 20.41Found(%): C, 53.56; H, 5.32; N, 2.92;S, 20.17 I-5A-55a ¹H-NMR(CDCl₃) δ 1.02(1H, m), 1.25–1.48(8H, m),1.55–1.66(4H, m), 2.01(1H, m), 2.32 (2H, dt, J=2.1, 7.5Hz), 2.38(3H, s),2.50(1H, brs), 3.80(1H, m), 5.99(1H, m), 6.07(1H, brd, J=5.7Hz),6.20(1H, t, J=3.3Hz), 7.18(1H, dd, J=1.8, 3.3Hz), 7.35(1H, d, J=3.9Hz),7.54(1H, d, J=3.9Hz); IR(CHCl₃)3514, 3442, 3149, 3101, 1709, 1657, 1529,1504, 1375, 1182, 1161, 1053cm⁻¹; [α]_(D) ²⁴+47.1±0.9°(c=1.003,MeOH)Anal. (C₂₂H₂₈N₂O₅S₂)Calcd.(%): C, 56.87; H, 6.07; N, 6.03; S,13.80Found(%): C, 56.59; H, 6.06; N, 5.91; S, 13.52 I-5A-59a¹H-NMR(CDCl₃) δ 0.97(1H, m), 1.16–1.68(12H, m), 1.98 (1H, d, J=3.9Hz),2.31(2H, t, J=7.5Hz), 2.47(1H, m), 3.79(1H, m), 5.86(1H, d, J=4.5Hz),7.01(1H, dd, J= 5.4, 3.6Hz), 7.04(1H, d, J=3.6Hz), 7.28(1H, dd, J= 3.6,1.2Hz), 7.31(1H, d, J=3.6Hz), 7.42(1H, dd, J= 5.4, 1.2Hz);IR(CHCl₃)3516, 3444, 3425, 2671, 1709, 1645, 1531, 1498, 1421cm⁻¹;[α]_(D) ^(25.0)+49.1±0.9°(c=1.003,MeOH)Anal.(C₂₁H₂₅NO₃S₃·0.1H₂O)Calcd.(%): C, 57.66; H, 5.81; N, 3.20; S,21.99Found(%): C, 57.47; H, 5.81; N, 3.23; S, 22.21 I-5A-59b¹H-NMR(CDCl₃) δ 0.96(1H, m), 1.16–1.66(12H, m), 1.98 (1H, d, J=3.6Hz),2.27(2H, dt, J=7.2, 1.8Hz), 2.49 (1H, m), 3.62(3H, s), 3.77(1H, m),5.85(1H, d, J=6.9Hz), 7.01(1H, dd, J=5.4, 3.6Hz), 7.04(1H, d, J=4.2Hz),7.29(1H, dd, J=3.6, 1.2Hz), 7.31(1H, d, J=4.2Hz), 7.43(1H, dd, J=5.4,1.2Hz) I-5A-88a ¹H-NMR(CDCl₃) δ 0.96(1H, m), 1.16–1.70(12H, m), 1.99(1H, d, J=3.6Hz), 2.32(2H, t, J=7.5Hz), 2.50(1H, m), 3.82(1H, m),4.16(2H, s), 5.85(1H, d, J=8.1Hz), 6.79 (1H, d, J=3.6Hz), 6.96(1H, dd,J=5.1, 1.5Hz), 7.05 (1H, m), 7.28(1H, dd, J=5.1, 3.0Hz), 7.35(1H, d, J=3.6Hz); IR(CHCl₃)3516, 3446, 3427, 1709, 1641, 1545, 1506, 1458cm⁻¹;[α]_(D) ^(24.0)+44.9±0.9°(c=1.003, MeOH)Anal.(C₂₂H₂₇NO₃S₂·0.1H₂O)Calcd.(%): C, 63.00; H, 6.54; N, 3.34; S,15.29Found(%): C, 63.06; H, 6.53; N, 3.43; S, 15.01

TABLE 19 Compd. No.. Physical property I-5A-104a ¹H-NMR(CDCl₃) δ0.99(1H, m), 1.18–1.70(12H, m), 1.99 (1H, m), 2.33(2H, t, J=7.5Hz),2.50(1H, m), 3.82(1H, m), 4.10(2H, s), 5.88(1H, d, J=8.4Hz), 6.70(1H, d,J= 3.6Hz), 6.95(1H, dd, J=5.4, 3.6Hz), 7.04(1H, dd, J= 3.6, 1.2Hz),7.28(1H, d, J=3.6Hz), 7.36(1H, dd, J=5.4, 1.2Hz); IR(CHCl₃)3514, 3446,2669, 1709, 1643, 1543, 1506, 1458cm⁻¹; [α]_(D) ^(25.0)+44.5±1.3°(c=0.670, MeOH)Anal. (C₂₂H₂₇NO₃S₃·0.2H₂O)Calcd.(%): C, 58.30; H, 6.09;N, 3.09; S, 21.22Found(%): C, 58.34; H, 6.09; N, 3.25; S, 21.10I-5A-143a ¹H-NMR(CDCl₃) δ 1.01(1H, m), 1.16–1.72(12H, m), 2.00 (1H, m),2.33(2H, t, J=7.5Hz), 2.57(1H, m), 3.93(1H, m), 4.24(2H, s), 6.03(1H, d,J=7.5Hz), 7.18–7.34(6H, m), 7.42(1H, t, J=7.8Hz), 7.80 (1H, s), 8.17(1H,d, J=7.8Hz); IR(CHCl₃)3514, 3438, 1709, 1651, 1516, 1495cm⁻¹; [α]_(D)^(24.0)+41.4±0.8°(c=1.000, MeOH)Anal.(C₂₈H₃₁NO₃S· 0.3H₂O)Calcd.(%): C,72.01; H, 6.82; N, 3.00; S, 6.87 Found(%): C, 72.05; H, 6.81; N, 3.02;S, 6.75 I-5A-197a ¹H-NMR(CDCl₃) δ 0.96(1H, m), 1.18–1.68(12H, m), 1.97(1H, d, J=3.9Hz), 2.32(2H, t, J=7.5Hz), 2.48(1H, m), 3.22(2H, t,J=8.7Hz), 3.80(1H, m), 4.07(2H, s), 4.57 (2H, t, J=8.7Hz), 5.83(1H, d,J=7.8Hz), 6.79(1H, t, J= 7.5Hz), 6.81(1H, d, J=3.9Hz), 6.97(1H, d,J=7.5Hz), 7.09(1H, d, J=7.5Hz), 7.33(1H, d, J=3.9Hz); IR (CHCl₃)3516,3446, 3427, 2679, 1709, 1641, 1543, 1506, 1458cm⁻¹; [α]_(D)^(25.0)+14.7±0.5° (c=1.009, MeOH)Anal. (C₂₆H₃₁NO₄S·0.6H₂O)Calcd.(%): C,67.24; H, 6.99; N, 3.01; S, 6.90Found(%): C, 67.14; H, 6.85; N, 3.03; S,6.64 I-5B-1a ¹H-NMR(CDCl₃) δ 1.08–1.70(7H, m), 2.04(1H, m), 2.10–2.18(2H, m), 2.53(1H, brs), 3.14(1H, d, J=6.0Hz), 3.81 (1H, m),5.52–5.67(2H, m), 6.25 (1H, d, J=6.9Hz), 6.33–6.34 (2H, m),7.14–7.16(2H, m), 7.35(1H, d, J=3.9Hz), 7.54(1H, d, J=3.9Hz);IR(CHCl₃)3512, 3440, 1712, 1658, 1531, 1504, 1456, 1383, 1192, 1167,1057, 1034cm⁻¹; [α]_(D) ²⁷+61.4±1.0°(c=1.008, MeOH)Anal.(C₂₁H₂₄N₂O₅S₂·0.3H₂O)Calcd.(%): C, 55.56; H, 5.46; N, 6.17; S,14.13Found(%): C, 55.47; H, 5.42; N, 6.54; S, 14.26 I-5C-1amp149–152°C.; ¹H-NMR(CDCl₃) δ 1.07(1H, m), 1.24–1.32(2H, m),1.41–1.48(2H, m), 1.53–1.69(4H, m), 2.01(1H, m), 2.23–2.30(2H, m),2.49(1H, brs), 3.87(1H, m), 5.78(1H, d, J=15.6Hz), 6.15(1H, d, J=7.2Hz),6.33–6.34(2H, m), 7.02(1H, dt, J=15.6and7.2Hz), 7.15–7.17(2H, m), 7.37and7.56(each1H, eachd, eachJ=4.2Hz); IR(CHCl₃) 3523, 3440, 2679, 1695,1655, 1529, 1504, 1456, 1383, 1192, 1167, 1057, 1034cm⁻¹; [α]_(D)²⁴+38.7±0.8°(c=1.001, MeOH)Anal.(C₂₁H₂₄N₂O₅S₂·0.2H₂O)Calcd.(%): C,55.78; H, 5.44; N, 6.20; S, 14.18Found(%): C, 55.70; H, 5.36; N, 6.20;S, 14.08

TABLE 20 Compd. No.. Physical property I-5C-31a ¹H-NMR(CDCl₃) δ 0.99(1H,m), 1.22–1.29(2H, m), 1.42–1.49(2H, m), 1.53–1.69(4H, m), 1.99(1H, m),2.18–2.33(2H, m), 2.49(1H, brs), 3.88(1H, m), 4.14(2H, s), 5.79(1H, d,J=15.6Hz), 5.85(1H, d, J=7.8Hz), 6.78 (1H, d, J=3.6Hz), 7.03(1H, dt,J=6.9and15.6Hz), 7.23–7.33(5H, m), 7.36(1H, d, J=3.6Hz); IR(CHCl₃) 3523,3446, 3427, 2679, 1695, 1649, 1543, 1506, 1456, 1308, 1282cm⁻¹; [α]_(D)²⁴+41.2±0.8° (c=1.011, MeOH) Anal.(C₂₄H₂₇NO₃S·0.2H₂O)Calcd.(%): C,69.77; H, 6.68; N, 3.39; S, 7.76Found(%): C, 69.72; H, 6.55; N, 3.40; S,7.65 I-5C-47a ¹H-NMR(CDCl₃) δ 1.09(1H, m), 1.25–1.31(2H, m),1.42–1.47(2H, m), 1.56–1.64(4H, m), 2.00(1H, m), 2.24–2.31(2H, m),2.49(1H, brs), 3.88(1H, m), 5.78(1H, d, J=15.6Hz), 6.25(1H, d, J=8.1Hz),7.02(1H, dt, J= 15.6and6.8Hz), 7.12(1H, dd, J=3.6and4.8Hz), 7.42and7.61(each1H, eachd, eachJ=3.9Hz), 7.70(1H, dd, J=1.5and4.8Hz),7.75(1H, dd, J=1.5and3.6Hz); IR (CHCl₃)3523, 3440, 3373, 2681, 1695,1653, 1529, 1504, 1335, 1402, 1153, 1095, 1020cm⁻¹; [α]_(D) ²⁴+39.1±0.8°(c=1.000, MeOH)Anal. (C₂₁H₃₃NO₅S₃·0.3H₂O)Calcd.(%): C, 53.55; H, 5.05;N, 2.97; S, 20.42Found(%): C, 53.58; H, 4.97; N, 3.04; S, 20.17 I-5C-88a¹H-NMR(CDCl₃) δ 1.00(1H, m), 1.23–1.30(2H, m), 1.43–1.48(2H, m),1.53–1.69(4H, m), 2.00(1H, m), 2.19–2.33(2H, m), 2.50(1H, brs), 3.88(1H,m), 4.16(2H, s), 5.79(1H, dt, J=15.6and1.5Hz), 5.90(1H, d, J=8.1Hz),6.79(1H, d, J=3.6Hz), 6.95–7.08(3H, m), 7.28(1H, dd, J=2.7and4.8Hz),7.36(1H, d, J=3.6Hz); IR (CHCl₃)3523, 3446, 3427, 2679, 1695, 1649,1543, 1506, 1458, 1284cm⁻¹; [α]_(D) ²⁴+39.9±0.8° (c=1.011, MeOH)Anal.(C₂₄H₂₇NO₃S·0.2H₂O)Calcd.(%): C, 63.04; H, 6.11; N, 3.34; S,15.30Found(%): C, 63.12; H, 5.96; N, 3.44; S, 15.22 I-5D-1amp150–152°C.; ¹H-NMR(CDCl₃) δ 1.32–1.66(6H, m), 1.96(1H, m),2.12–2.46(5H, m), 2.61(1H, brs), 3.87 (1H, m), 5.28(1H, m), 5.41(1H, dd,J=9.6, 10.5Hz), 6.33(2H, t, J=2.4Hz), 6.68(1H, br d, J=7.2Hz), 7.15 (2H,t, J=2.4Hz), 7.44(1H, d, J=3.9Hz), 7.48(1H, d, J= 3.9Hz); IR(CHCl₃)3510,3390, 3145, 3101, 2673, 1709, 1655, 1531, 1506, 1456, 13811192, 1167,1057, 1034cm⁻¹; [α]_(D) ²⁵+9.2±0.5° (c=1.011, MeOH)Anal.(C₂₁H₂₄N₂O₅S₂)Calcd.(%): C, 56.23; H, 5.39; N, 6.25; S, 14.30Found(%):C, 56.20; H, 5.44; N, 6.23; S, 14.23

TABLE 21 Compd. No.. Physical property I-5E-1a mp155–159°C.;¹H-NMR(CDCl₃) δ 1.18–1.82(9H, m), 2.00(1H, m), 2.61(1H, m),3.50–3.59(2H, m), 3.79(1H, m), 3.99and4.10(each1H, Abq, J=17.1Hz),5.54–5.70 (2H, m), 6.32–6.34(2H, m), 6.47(1H, d, J=6.3Hz), 7.14–7.17(2H,m), 7.39(1H, d, J=4.2Hz), 7.54(1H, d, J= 4.2Hz); IR(CHCl₃)3423, 1764,1730, 1655, 1531, 1506, 1456, 1383, 1192, 1167, 1057cm⁻¹; [α]_(D) ²³⁺28.9±0.7°(c=1.011, MeOH)Anal.(C₂₀H₂₆N₂O₆S₂) Calcd.(%): C, 53.08; H,5.35; N, 6.19; S, 14.17Found(%): C, 53.44; H, 5.62; N, 6.00; S, 13.70I-6A-1a mp109–111°C.; ¹H-NMR(CDCl₃) δ 1.02(1H, m), 1.24–1.56 (14H, m),1.98(1H, brs), 2.29(2H, t, J=7.2Hz), 2.48(1H, brs), 3.79(1H, m),6.28(1H, d, J=7.2Hz), 6.33(2H, t, J=2.4Hz), 7.15(2H, t, J=2.4Hz), 7.38and 7.55(each1H, eachd, eachJ=4.2Hz); IR(KBr)3352, 1709, 1624, 1541,1512, 1456, 1377, 1192, 1167, 1057, 1036cm⁻¹; [α]_(D) ^(24.5)+47.7±0.9°(c=1.003, MeOH)Anal. (C₂₂H₂₈N₂O₅S₂·0.2H₂O)Calcd.(%): C, 56.44; H, 6.11;N, 5.98; S, 13.70Found(%): C, 56.50; H, 6.11; N, 6.18; S, 13.51 I-6B-1a¹H-NMR(CDCl₃) δ 1.08(1H, m), 1.21–1.31(2H, m), 1.40–1.45(2H, m),1.58–1.66(2H, m), 2.03–2.19(3H, m), 2.32–2.46(4H, m), 2.52(1H, brs),3.80(1H, m), 5.33–5.45 (2H, m), 6.24(1H, d, J=7.8Hz), 6.32–6.34(2H, m),7.15–7.16(2H, m), 7.36(1H, d, J=3.9Hz), 7.55(1H, d, J= 3.9Hz);IR(CHCl₃)3514, 3440, 1711, 1657, 1531, 1504, 1456, 1383, 1192, 1167,1057, 1034cm⁻¹; [α]_(D) ^(24.5+) 69.8±1.1°(c=1.006, MeOH)Anal.(C₂₂H₂₆N₂O₅S₂·0.2H₂O)Calcd.(%): C, 56.68; H, 5.71; N, 6.01; S,13.76Found(%): C, 56.67; H, 5.70; N, 6.14; S, 13.89 I-6B-31a¹H-NMR(CDCl₃) δ 1.04(1H, m), 1.17–1.28(2H, m), 1.41–1.46(2H, m),1.55–1.66(2H, m), 2.00(1H, m), 2.04–2.24(2H, m), 2.31–2.44(4H, m),2.51(1H, brs), 3.82 (1H, m), 4.13(2H, s), 5.32–5.44(2H, m), 5.96(1H, d,J= 6.6Hz), 6.76(1H, dt, J=3.6and0.9Hz), 7.22–7.35(5H, m), 7.36(1H, d,J=3.6Hz); IR(CHCl₃)3514, 3444, 3427, 2671, 1711, 1643, 1545, 1506, 1454,1309, 1279cm⁻¹; [α]_(D) ²⁴+67.7±1.1°(c=1.002, MeOH)Anal.(C₂₅H₂₉NO₃S)Calcd.(%): C, 70.89; H, 6.90; N, 3.31; S, 7.57Found(%): C,70.67; H, 6.95; N, 3.36; S, 7.42 I-6D-1a ¹H-NMR(CDCl₃) δ 1.26–1.34(2H,m), 1.43–1.48(2H, m), 1.55–1.76(4H, m), 1.96–2.13(4H, m), 2.32(2H, t,J=7.2Hz), 2.59(1H, br s), 3.92(1H, m), 5.28–5.44(2H, m), 6.33 (2H, t,J=2.1Hz), 6.69(1H, br d, J=6.6Hz), 7.15(2H, t, J=2.1Hz), 7.39(1H, d,J=4.2Hz), 7.53(1H, d, J= 4.2Hz); IR(CHCl₃)3512, 3368, 1706, 1654, 1532,1506, 1455, 1382, 1212, 1132, 1106, 1075, 1016cm⁻¹; Anal.(C₂₂H₂₆N₂O₅S₂)Calcd.(%): C, 57.12; H, 5.67; N, 6.06; S, 13.86Found(%):C, 56.91; H, 5.71; N, 6.18; S, 13.75

TABLE 22 Compd. No.. Physical property I-7A-1a mp114–117°C.;¹H-NMR(CDCl₃) δ 1.05(1H, m), 1.18–1.70 (16H, m), 2.00(1H, m), 2.32(2H,t, J=6.9Hz), 2.49 (1H, m), 3.80(1H, m), 6.05(1H, d, J=7.2Hz), 6.32–6.35(2H, m), 7.15–7.18(2H, m), 7.35(1H, d, J=3.9Hz), 7.57 (1H, d, J=3.9Hz);IR(CHCl₃)3442, 1708, 1657, 1529, 1504, 1456, 1383, 1192, 1167, 1057,1034cm⁻¹; [α]_(D) ²⁴⁺ 45.9±0.9°(c=1.004, MeOH)Anal.(C₂₃H₃₀N₂O₅S₂)Calcd.(%): C, 57.72; H, 6.32; N, 5.85; S, 13.40Found (%): C, 57.56; H,6.44; N, 5.82; S, 13.11 I-7A-1e ¹H-NMR(CDCl₃) δ 1.01(1H, m),1.29–1.67(16H, m), 1.99 (1H, m), 2.30(2H, t, J=7.2Hz), 2.45(1H, m),3.28(3H, s), 3.84(1H, m), 6.14(1H, d, J=7.8Hz), 6.34(2H, d, J= 4.5Hz),7.16(2H, d, J=4.5Hz), 7.40(1H, d, J=3.9Hz), 7.58(1H, d, J=3.9Hz);IR(CHCl₃)3386, 2954, 2929, 2877, 2858, 1720, 1651, 1531, 1506, 1456,1425, 1398, 1385, 1342, 1167, 1076, 1067, 1034cm⁻¹; [α]_(D) ²⁵⁺38.5±0.8°(c=1.01, MeOH)Anal. (C₂₄H₃₃N₃O₆S₃·0.8MeOH)Calcd.(%): C, 51.24;H, 6.28; N, 7.23; S, 16.55Found(%): C, 51.59; H, 6.17; N, 7.40; S, 16.22I-7A-1h mp134–136°C.; ¹H-NMR(CDCl₃) δ 0.97(1H, m), 1.28–1.69 (18H, m),2.01(1H, m), 2.49(1H, brs), 3.61(2H, t, J= 6.6Hz), 3.81(1H, m), 6.05(1H,d, J=7.8Hz), 6.33–6.35 (2H, m), 7.16–7.17(2H, m), 7.35and7.57(each1H,eachd, eachJ=3.9Hz); IR(Nujol)3357, 3244, 1621, 1554, 1371, 1186, 1169,1061, 1038cm⁻¹; [α]_(D) ²⁴⁺ 47.8±0.9°(c=1.005, MeOH)Anal.(C₂₃H₃₂N₂O₄S₂·0.2AcOEt)Calcd.(%): C, 59.27; H, 7.02; N, 5.81; S,13.30Found(%): C, 59.53; H, 7.09; N, 5.92; S, 13.29 I-7A-1i mp82–84°C.;¹H-NMR(CDCl₃) δ 0.95(1H, m), 1.26–1.65 (18H, m), 2.01(1H, m), 2.49(1H,brs), 3.32(3H, s), 3.34 (2H, t, J=6.6Hz), 3.80(1H, m), 5.97(1H, d,J=7.5Hz), 6.33–6.34(2H, m), 7.16–7.17(2H, m), 7.33and7.58(each 1H,eachd, eachJ=3.9Hz); IR(CHCl₃)3442, 1658, 1529, 1504, 1456, 1385, 1192,1167, 1113, 1057, 1034cm⁻¹; [α]_(D) ²⁵+43.9±0.8°(c=1.003, MeOH)Anal.(C₂₄H₃₄N₂O₄S₂)Calcd.(%): C, 60.22; H, 7.16; N, 5.85; S, 13.40Found(%):C, 60.27; H, 7.14; N, 5.79; S, 13.29 I-7A-31a ¹H-NMR(CDCl₃) δ 0.92(1H,m), 1.18–1.66(16H, m), 1.96 (1H, m), 2.31(2H, t, J=7.5Hz), 2.48(1H, m),3.81(1H, m), 4.13(2H, s), 5.83(1H, d, J=8.1Hz), 6.77(1H, d, J= 3.9Hz),7.21–7.36(6H, m); IR(CHCl₃)3516, 3446, 3427, 1709, 1643, 1543, 1506,1456cm⁻¹; [α]_(D) ^(24.0)+41.0±0.8° (c=1.006,MeOH)Anal.(C₂₆H₃₃NO₃S·0.2H₂O)Calcd.(%): C, 70.46; H, 7.60; N, 3.16; S,7.23Found(%): C, 70.43; H, 7.66; N, 3.21; S, 7.07

TABLE 23 Compd. No.. Physical property I-7A-47a ¹H-NMR(CDCl₃) δ 0.98(1H,m), 1.16–1.70(16H, m), 1.99 (1H, m), 2.31(2H, t, J=7.5Hz), 2.49(1H, m),3.80(1H, m), 6.05(1H, d, J=7.8Hz), 7.10(1H, dd, J=4.8, 3.6Hz), 7.39(1H,d, J=3.9Hz), 7.64(1H, d, J=3.9Hz), 7.69(1H, dd, J=4.8, 1.2Hz), 7.75(1H,dd, J=3.6, 1.2Hz); IR (CHCl₃)3514, 3442, 3375, 2677, 1709, 1655, 1529,1504, 1402, 1336, 1153, 1095, 1022cm⁻¹; [α]_(D) ^(24.0)+45.7±0.9°(c=1.010, MeOH)Anal.(C₂₃H₂₉NO₅S₃·0.2H₂O)Calcd.(%): C, 55.33; H, 5.94; N,2.80; S, 19.26Found(%): C, 55.42; H, 6.04; N, 2.86; S, 19.03 I-7A-47i¹H-NMR(CDCl₃) δ 0.96(1H, m), 1.26–1.35(11H, m), 1.40–1.46 (2H, m),1.51–1.67(5H, m), 2.01(1H, m), 2.50(1H, brs), 3.32(3H, s), 3.34(2H, t,J=6.9Hz), 3.80(1H, m), 6.03(1H, d, J=7.5Hz), 7.11(1H, dd,J=3.9and4.8Hz), 7.38and7.65(each1H, eachd, eachJ=3.9Hz), 7.70(1H, dd,J=1.5and4.8Hz), 7.76(1H, dd, J=1.5and3.9Hz); IR(CHCl₃)3442, 1657, 1529,1504, 1402, 1336, 1153, 1113, 1095, 1020cm⁻¹; [α]_(D) ²⁵+43.7±0.8°(c=1.008, MeOH)Anal. (C₂₄H₃₃NO₄S₃·0.1H₂O)Calcd.(%): C, 57.94; H, 6.73;N, 2.82; S, 19.34Found(%): C, 57.81; H, 6.68; N, 2.90; S, 19.42 I-7A-59a¹H-NMR(CDCl₃) δ 0.93(1H, m), 1.16–1.68(16H, m), 1.98 (1H, d, J=3.6Hz),2.31(2H, t, J=7.2Hz), 2.47(1H, m), 3.78(1H, m), 5.87(1H, d, J=7.5Hz),7.00(1H, dd, J=5.7, 3.9Hz), 7.04(1H, d, J=3.6Hz), 7.28(1H, dd, J=3.9,1.2Hz), 7.31(1H, d, J=3.6Hz), 7.42(1H, dd, J=5.7, 1.2Hz); IR(CHCI₃)3516,3444, 3427, 2671, 1709, 1645, 1529, 1498, 1421cm⁻¹; [δ ]_(D)^(25.0)+41.2±0.8° (c=1.003, MeOH)Anal. (C₂₃H₂₉NO₃S₃)Calcd.(%): C, 59.58;H, 6.30; N, 3.02; S, 20.75Found(%): C, 59.70; H, 6.27; N, 3.03; S, 20.56I-7A-88a ¹H-NMR(CDCl₃) δ 0.93(1H, m), 1.16–1.68(16H, m), 1.98 (1H, d,J=3.6Hz), 2.31(2H, t, J=7.5Hz), 2.49(1H, m), 3.81(1H, m), 4.15(2H, s),5.86(1H, d, J=7.5Hz), 6.79 (1H, d, J=3.6Hz), 6.96(1H, dd, J=4.8, 1.2Hz),7.05(1H, dd, J=3.0, 1.2Hz), 7.28(1H, dd, J=4.8, 3.0Hz), 7.35(1H, d,J=3.6Hz); IR(CHCl₃)3516, 3446, 3427, 1709, 1641, 1545, 1506, 1458cm⁻¹;[α]_(D) ^(24.0)+40.2±0.8° (c=1.007, MeOH)Anal.(C₂₄H₃₁NO₃S₂·0.1H₂O)Calcd.(%): C, 64.42; H, 7.03; N, 3.13; S,14.33Found(%): C, 64.52; H, 7.00; N, 3.18; S, 14.04 I-7A-88h mp92–93°C.;¹H-NMR(CDCl₃) δ 0.94(1H, m), 1.20–1.34 (11H, m), 1.42–1.47(2H, m),1.48–1.63(5H, m), 1.98(1H, m), 2.49(1H, brs), 3.61(2H, t, J=6.6Hz),3.83(1H, m), 4.16(2H, s), 5.86(1H, d, J=8.1Hz), 6.79(1H, d, J= 3.6Hz),6.97(1H, dd, J=1.2and4.8Hz), 7.06(1H, m), 7.29 (1H, dd, J=3.0and4.8Hz),7.35(1H, d, J=3.6Hz); IR (Nujol)3315, 3259, 1599, 1549, 1527, 1317cm⁻¹;[α]_(D) ²⁴⁺ 45.0±0.9°(c=1.001, MeOH)Anal.(C₂₄H₃₃NO₂S₂) Calcd.(%): C,66.78; H, 7.71; N, 3.24; S, 14.86Found(%): C, 66.85; H, 7.71; N, 3.37;S, 14.57

TABLE 24 Compd. No.. Physical property I-7A-88i mp47–48°C.;¹H-NMR(CDCl₃) δ 0.93(1H, m), 1.23–1.32 (11H, m), 1.41–1.46(2H, m),1.51–1.63(5H, m), 1.98(1H, m), 2.50(1H, brs), 3.31(3H, s), 3.34(2H, t,J=6.6Hz), 3.81(1H, m), 4.16(2H, s), 5.81(1H, d, J=7.2Hz), 6.79 (1H, d,J=3.9Hz), 6.97(1H, dd, J=0.9and4.8Hz), 7.06 (1H, m), 7.29(1H, dd,J=3.0and4.8Hz), 7.34(1H, d, J= 3.9Hz); IR(CHCl₃)3446, 3426, 1643, 1543,1506, 1460, 1113cm⁻¹; [α]_(D) ^(25.5)+43.0±0.8° (c=1.008, MeOH)Anal.(C₂₅H₃₅NO₂S₂)Calcd.(%): C, 67.37; H, 7.92; N, 3.14; S, 14.39Found(%): C,67.32; H, 7.91; N, 3.19; S, 14.32 I-7A-104a ¹H-NMR(CDCl₃) δ 0.95(1H, m),1.18–1.70(16H, m), 2.00 (1H, d, J=3.6Hz), 2.32(2H, t, J=7.5Hz), 2.50(1H,m), 3.82(1H, m), 4.10(2H, s), 5.87(1H, d, J=7.2Hz), 6.70 (1H, d,J=3.6Hz), 6.95(1H, dd, J=5.4, 3.6Hz), 7.04(1H, dd, J=3.6, 1.2Hz),7.28(1H, d, J=3.6Hz), 7.36(1H, dd, J= 5.4, 1.2Hz); IR(CHCl₃)3516, 3446,3427, 2671, 1709, 1643, 1543, 1506, 1458cm⁻¹; [α]_(D)^(25.0)+39.4±0.8°.(c=1.004, MeOH)Anal.(C₂₄H₃₁NO₃S₃)Calcd.(%): C, 60.34;H, 6.54; N, 2.93; S, 20.14Found(%): C, 60.12; H, 6.51; N, 3.05; S, 19.95I-7A-143a ¹H-NMR(CDCl₃) δ 0.97(1H, m), 1.16–1.70(16H, m), 2.00 (1H, m),2.31(2H, t, J=7.5Hz), 2.58(1H, m), 3.93(1H, m), 4.24(2H, s), 6.01(1H, d,J=7.2Hz), 7.18–7.32(6H, m), 7.42(1H, t, J=7.8Hz), 7.80(1H, s), 8.18(1H,d, J=7.2Hz); IR(CHCl₃)3516, 3438, 1709, 1651, 1516, 1495cm⁻¹; [α]_(D)^(24.0)+41.9±0.8°(c=1.006, MeOH)Anal. (C₃₀H₃₅NO₃S· 0.2H₂O)Calcd.(%): C,73.05; H, 7.23; N, 2.84; S, 6.50 Found(%): C, 73.10; H, 7.13; N, 2.86;S, 6.39 I-7A-197a ¹H-NMR(CDCl₃) δ 0.93(1H, m), 1.18–1.68(16H, m), 1.97(1H, d, J=3.9Hz), 2.31(2H, t, J=7.5Hz), 2.48(1H, m), 3.22(2H, t,J=9.0Hz), 3.81(1H, m), 4.07(2H, s), 4.57 (2H, t, J=9.0Hz), 5.82(1H, d,J=7.5Hz), 6.79(1H, t, J= 7.2Hz), 6.80(1H, d, J=7.2Hz), 6.96(1H, d,J=7.2Hz), 7.09(1H, d, J=7.2Hz), 7.33(1H, d, J=7.2Hz); IR (CHCl₃)3516,3446, 3427, 2671, 1709, 1641, 1543, 1506, 1458cm⁻¹; [α]_(D)^(25.0)+37.9±0.8° (c=1.003, MeOH)Anal. (C₂₈H₃₅NO₄S·0.3H₂O)Calcd.(%): C,69.05; H, 7.39; N, 2.88; S, 6.58Found(%): C, 69.11; H, 7.24; N, 2.99; S,6.61 I-7A-315a ¹H-NMR(CDCl₃) δ 1.00(1H, m), 1.23–1.63(16H, m), 2.00 (1H,m), 2.31(2H, t, J=7.2Hz), 2.58(1H, m), 3.94(1H, m), 4.26(2H, s),6.06(1H, d, J=7.8Hz), 7.00–7.18(5H, m), 7.42(1H, m), 7.82(1H, s),8.18(1H, d, J=7.2Hz); IR(CHCl₃)3516, 3438, 2954, 2927, 2875, 2856, 1709,1653, 1516, 1492, 1456, 1396, 1298, 1271cm⁻¹; [α]_(D) ^(25.5)+39.0±0.8°(c=1.04, MeOH)Anal.(C₃₀H₃₄FNO₃S·0.5MeOH)Calcd.(%): C, 69.95; H, 6.93; N,2.67; F, 3.63; S, 6.12Found(%): C, 70.24; H, 6.80; N, 2.98; F, 3.19; S,6.08

TABLE 25 Compd. No.. Physical property I-7A-316a ¹H-NMR(CDCl₃) δ0.98(1H, m), 1.22–1.63(16H, m), 2.00 (1H, m), 2.31(2H, t, J=7.5Hz),2.58(1H, m), 3.82(3H, s), 3.92(1H, m), 4.23(2H, s), 6.03(1H, d,J=8.1Hz), 6.85–6.91(2H, m), 7.02–7.23(3H, m), 7.39(1H, m), 7.83 (1H, s),8.14(1H, d, J=8.4Hz); IR(CHCl₃)3518, 3438, 2954, 2929, 1709, 1653, 1601,1516, 1493, 1464, 1439, 1394, 1246cm⁻¹; [α]_(D)^(26.0)+35.2±0.7°(c=1.03, MeOH) Anal.(C₃₁H₃₇NO₄S·0.2H₂O)Calcd.(%): C,71.15; H, 7.20; N, 2.68; S, 6.13Found(%): C, 71.03; H, 7.35; N, 2.86; S,5.99 I-7B-1a ¹H-NMR(CDCl₃) δ 0.98–2.49(20H, m), 1.14(3H, d, J= 6.9Hz),3.80(1H, m), 6.05(1H, d, J=5.2Hz), 6.33(2H, d, J=4.2Hz), 7.16(2H, d,J=4.2Hz), 7.35(1H, m), 7.57 (1H, m); IR(CHCl₃)3442, 2954, 2929, 2877,2858, 1705, 1657, 1529, 1504, 1456, 1383, 1167, 1057, 1034cm⁻¹; [α]_(D)^(24.5)+41.6±1.6°(c=0.50, CHCl₃)Anal. (C₂₄H₃₂N₂O₅S₂·0.4MeOH)Calcd.(%):C, 57.98; H, 6.70; N, 5.54; S, 12.69Found(%): C, 58.27; H, 6.47; N,5.50; S, 12.33 I-7D-1a ¹H-NMR(CDCl₃) δ 0.98(1H, m), 1.22–2.33(17H, m),2.48 (1H, m), 3.79(1H, m), 4.92(1H, dt, J=6.0and44.1Hz), 6.07(1H, d,J=7.2Hz), 6.33(2H, d, J=4.8Hz), 7.16 (2H, d, J=4.8Hz), 7.36(1H, d,J=3.6Hz), 7.57(1H, d, J=3.6Hz); IR(CHCl₃)3440, 2956, 2875, 1732, 1657,1531, 1504, 1456, 1383, 1167, 1057, 1034cm⁻¹; [α]_(D) ²⁵⁺30.2±0.7°(c=1.02, MeOH)Anal. (C₂₃H₂₉FN₂O₅S₂·0.3MeOH)Calcd.(%): C, 55.28;H, 6.01; N, 5.53; F, 3.75; S, 12.67Found(%): C, 55.58; H, 6.14; N, 5.61;S, 12.05 I-7E-1c ¹H-NMR(CDCl₃) δ 1.18–1.30(3H, m), 1.40–1.45(2H, m),1.57–1.82(5H, m), 1.95–2.28(6H, m), 2.54(1H, br s), 3.75(1H, m),5.26(1H, br), 5.30–5.46(2H, m), 5.89(1H, br), 6.33(2H, t, J=2.4Hz),6.69(1H, br d, J=6.0Hz), 7.17(2H, t, J=2.4Hz), 7.48(1H, d, J=3.9Hz),7.57 (1H, d, J=3.9Hz); IR(CHCl₃)3527, 3485, 3442, 3411, 3340, 1674,1531, 1504, 1456, 1383, 1192, 1167, 1057, 1034cm⁻¹; [α]_(D)²⁴+79.9±1.2°(c=1.002, MeOH)Anal. (C₂₃H₂₉N₃O₄S₂·0.3H₂O)Calcd.(%): C,57.43; H, 6.20; N, 8.74; S, 13.33Found(%): C, 57.55; H, 6.50; N, 8.76;S, 13.28 I-7E-1d ¹H-NMR(CDCl₃) δ 1.19–1.27(3H, m), 1.40–1.45(2H, m),1.56–1.82(5H, m), 1.97–2.20(6H, m), 2.56(1H, br s), 2.75 (3H, d,J=4.8Hz), 3.73(1H, m), 5.29–5.42(2H, m), 5.90 (1H, br), 6.33(2H, t,J=2.1Hz), 6.79(1H, br d, J=7.8Hz), 7.16(2H, t, J=2.1Hz),7.54and7.57(each1H, ABq, J=3.9Hz); [α]_(D) ²⁴+76.1±1.2°(c=1.006, MeOH)Anal.(C₂₄H₃₁N₃O₄S₂·0.3H₂O)Calcd.(%): C, 58.23; H, 6.43; N, 8.49; S,12.95Found(%): C, 58.22; H, 6.64; N, 8.45; S, 12.81

TABLE 26 Compd. No.. Physical property I-7E-1e ¹H-NMR(CDCl₃) δ1.16–2.24(13H, m), 2.32(2H, d, J= 7.2Hz), 2.57(1H, m), 3.27(3H, s),3.74(1H, m), 5.25–5.32 (2H, m), 6.14(1H, d, J=7.5Hz), 6.35(2H, d,J=4.8Hz), 7.18(2H, d, J=4.8Hz), 7.46(1H, d, J=3.9Hz), 7.60(1H, d,J=3.9Hz), 9.96(1H, s); IR(CHCl₃)2956, 2879, 1716, 1645, 1533, 1506,1456, 1385, 1342, 1167, 1122, 1057, 1034cm⁻¹; [α]_(D) ²⁴+90.4±1.3°(c=1.00, CHCl₃) Anal.(C₂₄H₃₁N₃O₆S₃·0.8MeOH)Calcd.(%): C, 51.41; H, 5.95;N, 7.25; S, 16.60Found(%): C, 51.77; H, 5.70; N, 7.53; S, 16.22 I-7E-1f¹H-NMR(CDCl₃) δ 1.07–2.19(13H, m), 2.51(1H, m), 2.58 (2H, t, J=7.5Hz),3.22(3H, s), 3.27(3H, s), 3.84(1H, m), 5.32–5.43(2H, m), 6.26(1H, d,J=7.8Hz), 6.33(2H, d, J=4.5Hz), 7.17(2H, d, J=4.5Hz), 7.39(1H, d, J=4.2Hz), 7.58(1H, d, J=4.2Hz); IR(CHCl₃)3394, 2956, 2877, 1699, 1655,1531, 1504, 1456, 1381, 1354, 1167, 1057, 1034cm⁻¹; [α]_(D)^(24.5)+47.4±0.9° (c=1.00, CHCl₃) Anal.(C₂₅H₃₃N₃O₆S₃·0.2H₂O)Calcd.(%):C, 52.55; H, 5.89; N, 7.35; S, 16.84Found(%): C, 52.85; H, 5.81; N,7.26; S, 16.45 I-7E-1g ¹H-NMR(CDCl₃) δ 1.12–1.86(9H, m), 2.01–2.10(5H,m), 2.55(1H, br s), 2.96–3.04(2H, m), 3.57(1H, m), 5.27–5.40 (2H, m),6.36(2H, t, J=2.1Hz), 7.17(2H, t, J=2.1Hz), 7.46(1H, d, J=3.9Hz),7.60(1H, d, J=3.9Hz); IR (CHCl₃)3462, 3336, 1657, 1531, 1506, 1456,1383, 1192, 1167, 1057, 1036cm⁻¹; [α]_(D) ²⁵+74.0±1.1°(c=1.000,MeOH)Anal.(C₂₃H₂₈N₆O₃S₂·0.4Et₂O)Calcd.(%): C, 55.72; H, 6.08; N, 15.85;S, 12.09Found(%): C, 55.45; H, 6.10; N, 15.85; S, 11.84 I-7E-1hmp123–125°C.; ¹H-NMR(CDCl₃) δ 1.09(1H, m), 1.16–1.75 (10H, m),1.99–2.20(5H, m), 2.52(1H, brs), 3.63 (2H, t, J=6.5Hz), 3.81(1H, m),5.28–5.44(2H, m), 6.24 (1H, d, J=7.2Hz), 6.33–6.34(2H, m), 7.15–7.17(2H,m), 7.37and7.57(each1H, eachd, eachJ=3.9Hz); IR (Nujol)3388, 3255, 1618,1552, 1373, 1190, 1163, 1057, 1039cm⁻¹; [α]_(D) ²⁵+80.1±1.2° (c=1.014,MeOH)Anal. (C₂₃H₃₀N₂O₄S₂)Calcd.(%): C, 59.71; H, 6.54; N, 6.06; S,13.86Found(%): C, 59.59; H, 6.50; N, 6.08; S, 13.82 I-7E-1i¹H-NMR(CDCl₃) δ 1.06(1H, m), 1.19–1.31(2H, m), 1.34–1.44(4H, m),1.52–1.65(4H, m), 2.01–2.13(5H, m), 2.53(1H, brs), 3.32(3H, s), 3.37(2H,t, J=6.3Hz), 3.82 (1H, m), 5.28–5.44(2H, m), 6.15(1H, d, J=7.5Hz),6.32–6.34(2H, m), 7.15–7.17(2H, m), 7.35and7.57(each 1H, eachd,eachJ=4.2Hz); IR(CHCl₃)3442, 1658, 1529, 1504, 1456, 1382, 1192, 1167,1115, 1057, 1034cm⁻¹; [α]_(D) ²⁴+73.8±1.1°(c=1.006, MeOH)Anal.(C₂₄H₃₂N₂O₄S₂·0.2H₂O)Calcd.(%): C, 60.02; H, 6.80; N, 5.83; S,13.35Found(%): C, 60.09; H, 6.75; N, 5.79; S, 13.19

TABLE 27 Compd. No.. Physical property I-7E-47i ¹H-NMR(CDCl₃) δ 1.08(1H,m), 1.21–1.31(2H, m), 1.21–1.31(2H, m), 1.37–1.46(4H, m), 2.01–2.13(5H,m), 2.53(1H, brs), 3.32(3H, s), 3.37(2H, t, J=6.6Hz), 3.82 (1H, m),5.28–5.43(2H, m), 6.19(1H, d, J=7.2Hz), 6.19 (1H, d, J=7.2Hz), 7.11(1H,dd, J=3.9and5.1Hz), 7.39and7.63(each1H, eachd, eachJ=3.9Hz), 7.69 (1H,dd, J=1.5and5.1Hz), 7.75 (1H, dd, J=1.5and3.9Hz); IR(CHCl₃)3442, 1657,1529, 1504, 1402, 1336, 1153, 1115, 1097, 1020cm⁻¹; [α]_(D)²⁴+76.3±1.2°(c=1.011, MeOH)Anal.(C₂₄H₃₁NO₄S₃·0.5H₂O)Calcd.(%): C, 57.34;H, 6.42; N, 2.79; S, 19.14Found(%): C, 57.25; H, 6.25; N, 2.83; S, 19.25I-7E-88e ¹H-NMR(CDCl₃) δ 1.11–1.66(9H, m), 1.93–2.34(7H, m), 2.59(1H,m), 3.24(3H, s), 3.70(1H, m), 4.17(2H, s), 5.21–5.31(2H, m), 5.92(1H, d,J=9.6Hz), 6.84(1H, d, J= 3.6Hz), 6.98(1H, dd, J=1.5and4.8Hz), 7.08(1H,dd, J=1.2and1.8Hz), 7.30(1H, m), 7.50(1H, d, J=3.6Hz), 10.78(1H, s);IR(CHCl₃)3444, 3425, 2954, 2877, 1714, 1630, 1545, 1510, 1456, 1408,1342, 1169, 1122cm⁻¹; [α]_(D) ²⁴+66.0±2.1°(c=0.50, MeOH)Anal.(C₂₅H₃₂N₂O₄S₃·0.3H₂O)Calcd.(%): C, 57.07; H, 6.25; N, 5.32; S,18.28Found(%): C, 57.38; H, 6.34; N, 5.52; S, 17.92 I-7E-88h¹H-NMR(CDCl₃) δ 1.04(1H, m), 1.19–1.75(10H, m), 2.02–2.24(5H, m),2.53(1H, brs), 3.63(2H, t, J=6.6Hz), 3.83(1H, m), 4.16(2H, s),5.30–5.44(2H, m), 5.90(1H, d, J=6.9Hz), 6.79(1H, d, J=3.6Hz), 6.96(1H,dd, J=1.5 and4.8Hz), 7.05(1H, dd, J=1.5and3.0Hz), 7.28(1H, dd,J=3.0and4.8Hz), 7.35(1H, d, J=3.6Hz); IR (CHCl₃)3624, 3446, 3429, 1643,1545, 1506cm⁻¹; [α]_(D) ²⁴⁺ 74.7±1.1°(c=1.009, MeOH)Anal.(C₂₄H₃₁NO₂S₂·0.2H₂O)Calcd.(%): C, 66.54; H, 7.31; N, 3.23; S,14.80Found(%): C, 66.55; H, 7.26; N, 3.38; S, 14.57 I-7E-88i¹H-NMR(CDCl₃) δ 1.03(1H, m), 1.18–1.29(2H, m), 1.34–1.47(4H, m),1.53–1.67(4H, m), 2.01–2.14(5H, m), 2.54(1H, brs), 3.32(3H, s), 3.36(2H,t, J=6.6Hz), 3.84 (1H, m), 4.16(2H, s), 5.29–5.43(2H, m), 5.90(1H, d, J=7.5Hz), 6.79(1H, dt, J=3.9and0.9Hz), 6.96(1H, dd, J= 1.5and5.1Hz),7.06(1H, m), 7.29(1H, dd, J=3.0and 5.1Hz), 7.35(1H, d, J=3.9Hz);IR(CHCl₃)3446, 3429, 1643, 1543, 1506, 1458, 1115cm⁻¹; [α]_(D)²⁵+68.1±1.1° (c=1.019, MeOH)Anal.(C₂₅H₃₃NO₂S₂·0.2H₂O)Calcd.(%): C,67.13; H, 7.53; N, 3.13; S, 14.34Found(%): C, 67.10; H, 7.53; N, 3.21;S, 14.32

TABLE 28 Compd. No.. Physical property I-7F-1a ¹H-NMR(CDCl₃) δ1.09–2.51(16H, m), 1.17(3H, m), 3.80 (1H, s), 5.28–5.42(2H, m), 6.24(1H,m), 6.33(2H, d, J= 4.5Hz), 7.15(2H, d, J=4.5Hz), 7.39(1H, d, J=4.2Hz),7.56(1H, d, J=4.2Hz); IR(CHCl₃)3442, 2956, 2877, 1705, 1657, 1531, 1504,1456, 1383, 1167, 1057, 1034cm⁻¹; [α]_(D) ²⁴+49.0±0.9°(c=1.00,CHCl₃)Anal. (C₂₄H₃₀N₂O₅S₂·0.7H₂O)Calcd.(%): C, 57.28; H, 6.29; N, 5.57;S, 12.74Found(%): C, 57.49; H, 6.11; N, 5.66; S, 12.46 I-7G-1a¹H-NMR(CDCl₃) δ 1.06–2.18(14H, m), 1.21(6H, s), 2.51 (1H, m), 2.75(1H,m), 5.27–5.43(2H, m), 6.17(1H, d, J= 6.9Hz), 6.33(2H, dd,J=4.5and2.4Hz), 7.16(2H, dd, J= 4.5and2.4Hz), 7.37(1H, d, J=4.2Hz),7.57(1H, d, J= 4.2Hz); IR(CHCl₃)3442, 2956, 2877, 1728, 1699, 1657,1531, 1504, 1475, 1456, 1383, 1167, 1074, 1057, 1034cm⁻¹; [α]_(D)²⁵+43.4±0.8°(c=1.00, CHCl₃) I-7G-88a ¹H-NMR(CDCl₃) δ 1.04–2.24(14H, m),1.20(3H, s), 1.21 (3H, s), 2.50(1H, m), 3.85(1H, m), 4.16(2H, s),5.29–5.43 (2H, m), 5.97(1H, d, J=7.5Hz), 6.79(1H, d, J=3.9Hz), 6.96(1H,dd, J=5.1and1.2Hz), 7.05(1H, d, J= 1.2Hz), 7.29(1H, m), 7.37(1H,J=3.9Hz); IR(CHCl₃) 3446, 3427, 2956, 2877, 1728, 1699, 1743, 1545,1506, 1475, 1458, 1282, 1024cm⁻¹; [α]_(D) ²⁶+48.6±0.9°(c=1.02,CHCl₃)Anal.(C₂₆H₃₃NO₃S₂·0.3H₂O)Calcd.(%): C, 65.46; H, 7.10; N, 2.94; S,13.44Found(%): C, 65.66; H, 6.96; N, 3.12; S, 13.05 I-7G-126a¹H-NMR(CDCl₃) δ 0.95(1H, d, J=9.9Hz), 1.08(3H, s), 1.17(3H, s), 1.90(3H,s), 1.21(3H, s), 1.53–2.51(12H, m), 3.84(3H, s), 4.12(2H, s), 4.24(1H,m), 5.39–5.43(2H, m), 6.04(1H, d, J=8.7Hz), 6.77(1H, d, J=2.7Hz),6.86–6.92(2H, m), 7.14–7.23(2H, m), 7.31(1H, d, J=3.6Hz); IR(CHCl₃)3450,3431, 2924, 1728, 1699, 1641, 1601, 1543, 1506, 1471, 1406, 1387, 1367,1319, 1288, 1126, 1049, 1030cm⁻¹; [α]_(D) ²⁵+29.7±0.7°(c=1.00, CHCl₃)Anal.(C₃₁H₄₁NO₄S·0.3H₂O)Calcd.(%): C, 70.37; H, 7.92; N, 2.65; S,6.06Found(%): C, 70.50; H, 8.03; N, 2.78; S, 5.84 I-7I-1a ¹H-NMR(CDCl₃)δ 0.98(1H, m), 1.19–1.49(10H, m), 1.54–1.67(2H, m), 2.00(1H, m),2.16–2.24(2H, m), 2.48 (1H, brs), 3.81(1H, m), 5.79(1H, d, J=15.6Hz),6.12 (1H, d, J=7.2Hz), 6.33–6.34(2H, m), 7.03(1H, dt, J= 15.6and7.2Hz),7.15–7.17(2H, m), 7.35and7.56(each 1H, eachd, eachJ=3.9Hz);IR(CHCl₃)3523, 3442, 2681, 1695, 1655, 1529, 1504, 1456, 1425, 1383,1192, 1167, 1057, 1034cm⁻¹; [α]_(D) ^(24.5)+40.1±0.8°(c=1.003,MeOH)Anal.(C₂₃H₂₈N₂O₅S₂·0.3H₂O)Calcd.(%): C, 57.31; H, 5.98; N, 5.81; S,13.30Found(%): C, 57.59; H, 5.98; N, 5.86; S, 14.04

TABLE 29 Compd. No.. Physical property I-7I-31a mp134–136°C.;¹H-NMR(CDCl₃) δ 0.94(1H, m), 1.18–1.46 (10H, m), 1.54–1.68(2H, m),1.98(1H, m), 2.16–2.23 (2H, m), 2.48(1H, brs), 3.83(1H, m), 4.14(2H, s),5.79 (1H, dt, J=15.6and1.5Hz), 5.83(1H, d, J=6.9Hz), 6.78(1H, d,J=3.3Hz), 7.03(1H, dt, J=6.8and15.6Hz), 7.23–7.33(5H, m), 7.35(1H, d,J=3.3Hz); IR(KBr) 3329, 1695, 1649, 1616, 1549, 1527, 1454, 1319,1288cm⁻¹; [α]_(D) ²⁵+35.6±0.8°(c=1.004, MeOH)Anal.(C₂₆H₃₁NO₃S)Calcd.(%): C, 71.36; H, 7.14; N, 3.20; S, 7.33Found(%): C,71.15; H, 7.14; N, 3.28; S, 7.22 I-7I-47a ¹H-NMR(CDCl₃) δ 1.00(1H, m),1.26–1.46(10H, m), 1.55–1.65(2H, m), 2.00(1H, m), 2.17–2.24(2H, m), 2.49(1H, brs), 3.82(1H, m), 5.79(1H, d, J=15.6Hz), 6.16 (1H, d, J=7.5Hz),7.03(1H, dt, J=15.6and7.1Hz), 7.11(1H, dd, J=3.6and4.8Hz),7.40and7.63(each1H, eachd, eachJ=3.9Hz), 7.70(1H, dd, J=1.2and4.8Hz),7.75(1H, dd, J=1.2and3.6Hz); IR(CHCl₃)3523, 3442, 3375, 2681, 1695,1653, 1529, 1504, 1402, 1336, 1402, 1153, 1095, 1022cm⁻¹; [α]_(D)²⁴+40.3±0.80°(c=1.015, MeOH)Anal.(C₂₃H₂₇NO₅S₃·0.2H₂O)Calcd.(%): C,55.55; H, 5.55; N, 2.82; S, 19.35Found(%): C, 55.52; H, 5.46; N, 2.92;S, 19.31 I-7I-88a ¹H-NMR(CDCl₃) δ 0.95(1H, m), 1.21–1.46(10H, m),1.55–1.68(2H, m), 1.98(1H, m), 2.16–2.33(2H, m), 2.49 (1H, brs),3.83(1H, m), 4.16(2H, s), 5.79(1H, d, J=15.6Hz), 5.88(1H, d, J=7.5Hz),6.79(1H, d, J=3.6Hz), 6.95–7.08(3H, m), 7.28(1H, dd, J=3.0and4.8Hz),7.35 (1H, d, J=3.6Hz); IR(CHCl₃)3523, 3446, 3427, 2679, 1695, 1647,1545, 1506, 1458, 1300, 1281cm⁻¹; [α]_(D) ²⁴+ 34.7±0.70°(c=1.004,MeOH)Anal.(C₂₄H₂₉NO₃S₂) Calcd.(%): C, 64.98; H, 6.59; N, 3.16; S,14.46Found(%): C, 64.71; H, 6.61; N, 3.24; S, 14.17 I-7I-93amp116–120°C.; ¹H-NMR(CDCl₃) δ 0.95(1H, m), 1.21–1.68 (12H, m), 1.98(1H,m), 2.17–2.23(2H, m), 2.48(1H, brs), 3.84(1H, m), 4.34(2H, s), 5.80(1H,br d, J=15.6Hz), 5.84(1H, d), 6.85(1H, br d, J=3.3Hz), 6.90(1H, m),6.95(1H, dd, J=3.6, 5.1Hz), 7.02(1H, dt, J=15.9, 6.9Hz), 7.19(1H, dd,J=1.2, 5.1Hz), 7.35(1H, d, J= 3.3Hz); IR(Nujol)3032, 1695, 1648, 1542,1506, 1458, 1223, 1213cm⁻¹; [α]_(D) ^(26.0)+37.6±0.80°(c=1.015, MeOH)Anal.(C₂₄H₂₉NO₃S₂·0.1H₂O)Calcd.(%): C, 64.72; H, 6.61; N, 3.14; S,14.40Found(%): C, 64.64; H, 6.58; N, 3.24; S, 14.50

TABLE 30 Compd. No.. Physical property I-7I-126a ¹H-NMR(CDCl₃) δ0.93(1H, m), 1.20–1.48(10H, m), 1.54–1.64 (2H, s), 1.97(1H, d, J=3.6Hz),2.19(2H, dd, J=13.8, 6.9Hz), 2.47(1H, m), 3.84(3H, s), 4.12(2H, s),5.80(1H, dt, J=15.6, 1.5Hz), 5.81(1H, d, J=6.9Hz), 6.78(1H, d, J=3.9Hz),6.86–6.93(2H, m), 7.01(1H, dt, J=15.6, 6.9Hz), 7.16 (1H, d, J=7.2Hz),7.22(1H, d, J=7.2Hz), 7.31(1H, d, J= 3.9Hz); IR(Nujol)3276, 3079, 3058,2678, 1691, 1604, 1552, 1456, 1319, 1247cm⁻¹; [α]_(D) ^(27.0)+34.3±0.70°(c=1.010, MeOH) Anal.(C₂₇H₃₃NO₄S)Calcd.(%): C, 69.35; H, 7.11; N, 3.00;S, 6.86Found(%): C, 69.19; H, 7.10; N, 3.12; S, 6.62 I-7I-143a¹H-NMR(CDCl₃) δ 1.00(1H, m), 1.21–1.50(10H, m), 1.59–1.65(2H, m),2.00(1H, m), 2.17–2.21(2H, m), 2.57(1H, brs), 3.94(1H, m), 4.24(2H, s),5.79(1H, d, J=15.6Hz), 6.07 (1H, d, J=7.8Hz), 7.03(1H, dt,J=15.6and7.2Hz), 7.18–7.30(6H, m), 7.42(1H, t, J=7.8Hz), 7.81(1H, s),8.18(1H, d, J= 7.8Hz); IR(CHCl₃)3523, 3438, 2683, 1695, 1651, 1516,1495cm⁻¹; [α]_(D) ²⁴+41.7±0.80°(c=1.002, MeOH)Anal. (C₃₀H₃₃NO₃S)Calcd.(%): C, 73.62; H, 6.84; N, 2.86; S, 6.55Found(%): C, 73.54; H,6.77; N, 2.92; S, 6.49 I-7I-270a ¹H-NMR(CDCl₃) δ 0.99(1H, m),1.18–1.70(12H, m), 2.01 (1H, brd), 2.17–2.24(2H, m), 2.42(6H, s),2.48(1H, brs), 3.81(1H, m), 5.79(1H, dt, J=15.6, 1.5Hz), 5.88(2H, s),6.05(1H, d, J=7.5Hz), 7.03(1H, dt, J=15.6, 6.9Hz), 7.35(1H, d, J=3.9Hz), 7.50(1H, d, J=3.9Hz); IR(CHCl₃)3525, 3442, 2677, 1695, 1655,1529, 1504, 1375, 1180, 1119cm⁻¹; [α]_(D) ²⁵+37.7±0.8°(c=1.009,MeOH)Anal. (C₂₅H₃₂N₂O₅S₂·0.3H₂O) Calcd.(%): C, 58.87; H, 6.44; N, 5.49;S, 12.57 Found(%): C, 58.99; H, 6.39; N, 5.51; S, 12.48 I-7I-307amp171–173°C.; ¹H-NMR(CDCl₃) δ 0.91(1H, m), 1.17–1.41(10H, m),1.50–1.59(2H, m), 1.93(1H, m), 2.12–2.19(2H, m), 2.44(1H, m), 3.78(1H,m), 3.97(3H, s), 4.59(2H, s), 5.77 (1H, d, J=15.6Hz), 5.81(1H, d,J=7.2Hz), 6.75(1H, d, J=3.6Hz), 7.01(1H, dt, J=15.6, 7.1Hz), 7.28(1H, d,J=3.6Hz), 7.25–7.36(3H, m), 7.46(1H, m), 7.78–7.82(1H, m), 7.92 (1H, d,J=8.7Hz); IR(Nujol)3365, 3059, 2638, 1689, 1622, 1552, 1527, 1516, 1464,1263, 1252, 1092cm⁻¹; [α]_(D) ^(25.5+) 31.6±0.7°(c=1.001, MeOH)Anal.(C₃₁H₃₅NO₄S)Calcd.(%): C, 71.92; H, 6.81; N, 2.71; S, 6.19Found(%): C,71.62; H, 6.90; N, 2.79; S, 6.20 I-7I-327a mp176–179°C.; ¹H-NMR(CDCl₃) δ0.98(1H, m), 1.20–1.70 (12H, m), 2.00(1H, d, J=3.6Hz), 2.16–2.24(2H, m),2.47 (1H, brs), 3.00(2H, t, J=8.4Hz), 3.80(1H, m), 3.98 (2H, t,J=8.4Hz), 5.79(1H, dt, J=1.8, 15.3Hz), 6.01(1H, d, J=7.8Hz),6.97–7.24(4H, m), 7.33(1H, d, J=4.2Hz), 7.46(1H, d, J= 4.2Hz), 7.58(1H,d, J=8.4Hz); IR(Nujol)3332, 2925, 2854, 1689, 1608, 1554, 1479, 1460,1365, 1238, 1161cm⁻¹; [α]_(D) ²⁶+36.3±0.8°(c=1.012%, MeOH);Anal.(C₂₇H₃₂N₂O₅S₂) Calcd.(%)C, 61.34; H, 6.10; N, 5.30; S,12.13Found(%)C, 61.08; H, 6.22; N, 5.24; S, 11.82

TABLE 31 Compd. No.. Physical property I-7I-332a mp136–139°C.;¹H-NMR(CDCl₃) δ 0.98(1H, m), 1.20–1.82 (14H, m), 2.01(1H, d, J=3.0Hz),2.21(2H, q, J= 6.9Hz), 2.48(1H, brs), 2.53(2H, t, J=6.6Hz), 3.53 (2H, t,J=6.3Hz), 3.79–3.87(3H, m), 5.79(1H, dt, J= 1.5, 15.6Hz), 6.01(1H, d,J=7.2Hz), 6.97–7.26(5H, m), 7.31(1H, d, J=3.9Hz), 7.77(1H, dd, J=0.9,7.8Hz); IR (Nujol)3371, 3325, 2922, 1728, 1693, 1614, 1549, 1342,1163cm⁻¹; [α]_(D) ²⁴+35.4±0.8° (c=1.009%, MeOH); Anal.(C₂₈H₃₄N₂O₅S₂)Calcd.(%)C, 61.97; H, 6.31; N, 5.16; S, 11.82Found(%)C,61.94; H, 6.47; N, 5.14; S, 11.69 I-7I-343a ¹H-NMR(CDCl₃) δ 1.07(1H, m),1.22–1.62(12H, m), 1.98 (1H, m), 2.22(1H, m), 2.54(1H, m), 3.94(1H, m),5.80 (1H, d, J=15.6Hz), 6.27(1H, d, J=8.1Hz), 7.02(1H, m), 7.45–7.60(5H,m), 7.89(1H, s), 7.99–8.05(3H, m), 8.59(1H, d, J=8.1Hz); IR(KBr)3381,3292, 3066, 2949, 2927, 2873, 1685, 1655, 1620, 1558, 1477, 1446, 1385,1319, 1308, 1284, 1244, 1230, 1209cm⁻¹; [α]_(D) ^(26.0)+32.6±1.5°(c=0.50, DMSO)Anal.(C₂₉H₃₁NO₅S₂·0.4H₂O) Calcd.(%): C, 63.92; H, 5.88; N,2.57; S, 11.77Found(%): C, 64.07; H, 5.82; N, 2.75; S, 11.41 I-7I-385a¹H-NMR(CDCl₃) δ 1.03(1H, m), 1.20–1.74(12H, m), 2.04 (1H, m),2.14–2.26(2H, m), 2.57(1H, m), 3.97(1H, m), 5.77(1H, d, J=15.6Hz),6.27(2H, t, J=2.4Hz), 6.37 (1H, d, J=8.4Hz), 7.02(1H, dt, J=15.6,6.9Hz), 7.22 (2H, t, J=2.4Hz), 7.57(1H, t, J=7.8Hz), 7.67(1H, d, J=7.8Hz), 8.37(1H, d, J=7.8Hz), 8.44(1H, s); IR (CHCl₃)3452, 3023, 2954,2877, 1695, 1650, 1516, 1456, 1373, 1282, 1188, 1163, 1057cm⁻¹; [α]_(D)^(22.0)+39.4 ±0.8° (c=1.017, MeOH)Anal.(C₂₇H₃₀N₂O₅S₂·0.1H₂O) Calcd.(%):C, 61.36; H, 5.76; N, 5.30; S, 12.14Found(%): C, 61.26; H, 5.89; N,5.11; S, 11.95 I-7I-389a mp140–143°C.; ¹H-NMR(CDCl₃) δ 0.96(1H, m),1.21–1.46(10H, m), 1.54–1.64(2H, m), 1.99(1H, m), 2.23(3H,s)+2.16–2.23(2H, m), 2.48(1H, m), 3.21(2H, t, J=8.7Hz), 3.81(1H, m),4.62(2H, t, J=8.7Hz), 5.79(1H, d, J=15.6Hz), 5.88(1H, d, J=7.8Hz),6.89(1H, s), 6.96 (1H, s), 7.02(1H, dd, J=15.6, 6.9Hz), 7.08(1H, d,J=3.9Hz), 7.35(1H, d, J=3.9Hz); IR(Nujol)3294, 3066, 2675, 1695, 1649,1604, 1550, 1512, 1327, 1203cm⁻¹; [α]_(D) ²⁵+29.2±0.7°(c=1.013,MeOH)Anal. (C₂₈H₃₃NO₄S₂)Calcd.(%): C, 65.72; H, 650; N, 2.74; S,12.53Found(%): C, 65.57; H, 6.62; N, 2.62; S, 12.37

TABLE 32 Compd. No.. Physical property I-7I-391a mp204–207°C.;¹H-NMR(CDCl₃) δ 1.01(1H, m), 1.25–1.46 (10H, m), 1.54–1.64(2H, m),2.00(1H, m), 2.17–2.23(2H, m), 2.31(3H, s), 2.48(1H, m), 3.18(2H, t,J=8.7Hz), 3.81 (1H, m), 4.71(2H, t, J=8.7Hz), 5.79(1H, d, J=15.6Hz),6.20(1H, d, J=7.8Hz), 7.02(1H, dt, J=15.6, 6.9Hz), 7.21 (1H, s),7.41(1H, d, J=3.9Hz), 7.50(1H, s), 7.70(1H, d, J=3.9Hz); IR(Nujol)3398,3197, 3086, 1716, 1689, 1639, 1541, 1313, 1151cm⁻¹; [α]_(D)²⁵+37.9±0.8°(c=1.005, MeOH) Anal.(C₂₈H₃₃NO₆S₂)Calcd.(%): C, 61.85; H,6.12; N, 2.58; S, 11.80Found(%): C, 61.61; H, 6.08; N, 2.50; S, 11.69I-7J-1a mp116–118°C.; ¹H-NMR(CDCl₃) δ 0.99(1H, m), 1.19–1.82(12H, m),1.79(3H, d, J=1.2Hz), 2.01(1H, m), 2.17(2H, brq, J=7.8Hz), 2.48(1H, m),3.82(1H, m), 6.00(1H, d, J= 7.8Hz), 6.32–6.35(2H, m), 6.85(1H, m),7.15–7.17(2H, m), 7.33(1H, d, J=3.9Hz), 7.63(1H, d, J=3.9Hz), 7.57 (1H,d, J=3.9Hz); IR(Nujol)3354, 3141, 3099, 3076, 2669, 2557, 1682, 1641,1624, 1539, 1390, 1375, 1302, 1190, 1167cm⁻¹; [α]_(D)²⁶37.1±0.6°(c=1.002, MeOH)Anal. (C₂₄H₃₀N₂O₅S₂)Calcd.(%): C, 58.75; H,6.16; N, 5.71; S, 13.07Found(%): C, 58.55; H, 6.14; N, 5.70; S, 12.89I-7K-1a mp168–171°C.; ¹H-NMR(CDCl₃) δ 0.99(1H, m), 1.20–1.82 (12H, m),2.01–2.20(3H, m), 2.12(3H, d, J=0.9Hz), 2.48 (1H, m), 3.82(1H, m),4.05(2H, s), 5.65(1H, s), 5.97(1H, d, J=7.5Hz), 6.33–6.35(2H, m),7.16–7.18(2H, m), 7.33 (1H, d, J=3.9Hz), 7.63(1H, d, J=3.9Hz), 7.58(1H,d, J= 3.9Hz); IR(Nujol)3330, 3086, 1693, 1633, 1614, 1544, 1456, 1377,1250, 1194, 1169, 1057cm⁻¹; [α]_(D) ²⁶+34.0±1.5° (c=0.509, MeOH)Anal.(C₂₄H₃₀N₂O₅S₂·0.6CHCl₃) Calcd.(%): C, 52.55; H, 5.49; N, 4.98; S, 11.41;Cl, 11.35 Found(%): C, 52.62; H, 5.19; N, 4.93; S, 11.11; Cl, 10.53I-7M-1a ¹H-NMR(CDCl₃) δ 1.00–1.70(13H, m), 2.01(1H, m), 2.47 (1H, m),3.52(2H, t, J=6.6Hz), 3.82(1H, m), 4.04(2H, s), 5.54–5.70(2H, m),6.13(1H, d, J=7.2Hz), 6.32–6.35(2H, m), 7.15–7.18(2H, m), 7.37(1H, d,J=4.2Hz), 7.57(1H, d, J=4.2Hz); IR(CHCl₃)3440, 1778, 1731, 1655, 1531,1504, 1456, 1383, 1192, 1167, 1128, 1057, 1034cm⁻¹; [α]_(D) ²⁴⁺40.9±0.8°(c=1.007, MeOH)Anal. (C₂₂H₂₈N₂O₆S₂·0.4H₂O) Calcd.(%): C, 54.17;H, 5.95; N, 5.74; S, 13.15Found(%): C, 54.51; H, 6.00; N, 5.58; S, 12.76I-7M-1e ¹H-NMR(CDCl₃) δ 1.02–1.70(13H, m), 2.02(1H, m), 2.48 (1H, m),3.31(3H, s), 3.50(2H, t, J=6.6Hz), 3.85(1H, m), 3.99(2H, s), 6.05(1H, d,J=8.1Hz), 6.34(2H, m), 7.16 (2H, m), 7.36(1H, d, J=3.9Hz), 7.58(1H, d,J=3.9Hz), 8.88(1H, s); IR(CHCl₃)3442, 3352, 2956, 2877, 1730, 1657,1531, 1504, 1456, 1423, 1402, 1385, 1350, 1167, 1076, 1057, 1034cm⁻¹;[α]_(D) ^(25.5)+35.6±0.8°(c=1.00, MeOH)Anal.(C₂₃H₃₁N₃O₇S₃·0.8MeOH)Calcd.(%): C, 48.29; H, 5.74; N, 7.34; S,16.81Found(%): C, 48.00; H, 5.68; N, 7.74; S, 17.12

TABLE 33 Compd. No.. Physical property I-7M-40a ¹H-NMR(CDCl₃) δ 1.03(1H,m), 1.22–1.74(12H, m), 2.01 (1H, m), 2.51(1H, brs), 3.54(2H, dt, J=1.5,6.3Hz), 3.91 (1H, m), 4.05(2H, s), 6.03(1H, d, J=8.1Hz), 7.25–7.64 (7H,m); IR(CHCl₃)2954, 1780, 1732, 1643, 1541, 1510, 1491, 1454, 1219, 1213,1132cm⁻¹; [α]_(D) ²⁵+50.9±0.9° (c=1.013%, MeOH);Anal.(C₂₄H₂₉NO₄S·0.5H₂O)Calcd.(%) C, 66.03; H, 6.93; N, 3.21; S,7.34Found(%)C, 66.14; H, 6.92; N, 3.26; S, 7.22 I-7M-43a mp132–134°C.;¹H-NMR(CDCl₃) δ 1.01(1H, m), 1.20–1.75 (12H, m), 2.01(1H, d, J=3.0Hz),2.47(1H, brs), 3.53(2H, t, J=6.0Hz), 3.79–3.96(5H, m), 4.05(2H, s),6.06(1H, d, J= 7.8Hz), 6.85(1H, dd, J=1.5, 8.1Hz), 6.96(1H, m), 7.11(1H, m), 7.29(1H, d, J=4.2Hz), 7.34(1H, d, J=4.2Hz), 7.83(1H, dd, J=1.5,8.1Hz); IR(Nujol)3325, 3084, 2924, 1730, 1612, 1562, 1491, 1460, 1369,1250, 1236, 1165, 1138cm⁻¹; [α]_(D) ²⁶+53.6±0.9° (c=1.009%, MeOH); Anal.(C₂₂H₂₇NO₄S₂)Calcd.(%)C, 60.94; H, 6.28; N, 3.23; S, 14.79Found(%)C,60.77; H, 6.32; N, 3.38; S, 14.51 I-7M-47a mp116–118°C.; ¹H-NMR(CDCl₃) δ1.06(1H, m), 1.19–1.70(12H, m), 2.00(1H, m), 2.49(1H, m), 3.52(2H, t,J=6.3Hz), 3.84(1H, m), 4.05(2H, s), 6.21(1H, d, J=7.8Hz), 7.11(1H, dd,J=3.9, 4.5Hz), 7.42(1H, d, J=3.9Hz), 7.63 (1H, d, J=3.9Hz), 7.70(1H, dd,J=0.9, 4.8Hz), 7.75(1H, dd, J=0.9, 3.9Hz); IR(Nujol)3319, 3097, 2557,1732, 1618, 1566, 1444, 1432, 1321, 1232, 1151, 1031cm⁻¹; [α]_(D) ²⁴+44.4±0.8°(c=1.009, MeOH)Anal.(C₂₂H₂₇NO₆S₃) Calcd.(%): C, 53.10; H, 5.47;N, 2.81; S, 19.33Found(%): C, 52.90; H, 5.37; N, 2.91; S, 19.10 I-7M-59amp103–104°C.; ¹H-NMR(CDCl₃) δ 0.99(1H, m), 1.20–1.70(12H, m), 1.99(1H,d, J=3.3Hz), 2.45(1H, m), 3.23(2H, t, J=8.7Hz), 3.48–3.55(2H, m),3.84(1H, m), 4.04(2H, s), 5.89(1H, d, J=8.1Hz), 7.01(1H, dd, J=3.6,5.1Hz), 7.04 (1H, d, J=3.9Hz), 7.29(1H, dd, J=1.5, 3.6Hz), 7.33(1H, d,J=3.9Hz), 7.43(1H, dd, J=1.5, 5.1Hz); IR(Nujol) 3332, 2922, 2854, 1930,1601, 1564, 1458, 1439, 1331, 1230, 1134cm⁻¹; [α]_(D)²⁶+40.0±0.8°(c=1.004%, MeOH); Anal.(C₂₂H₂₇NO₄S₃)Calcd.(%)C, 56.75; H,5.84; N, 3.01; S, 20.66Found(%)C, 56.59; H, 5.81; N, 3.04; S, 20.65I-7M-88a mp90–91.5°C.; ¹H-NMR(CDCl₃) δ 1.00(1H, m), 1.18–1.70 (12H, m),1.99(1H, m), 2.46(1H, m), 3.52(2H, dt, J=1.8, 8.7Hz), 387(1H, m),4.04and4.16(each2H, s), 4.58(1H, brs), 5.91(1H, d, J=8.7Hz), 6.80(1H, d,J=3.6Hz), 6.96 (1H, dd, J=1.2, 5.1Hz), 7.06(1H, m), 7.29(1H, dd, J= 3.0,4.8Hz), 7.37(1H, d, J=3.9Hz); IR(Nujol)3332, 3095, 3080, 2553, 1735,1597, 1562, 1537, 1435, 1325, 1304, 1228, 1146cm⁻¹; [α]_(D)²⁴+39.8±0.8°(c=1.002, MeOH)Anal. (C₂₃H₂₉NO₄S₂)Calcd.(%): C, 61.72; H,6.53; N, 3.13; S, 14.33Found(%): C, 61.60; H, 6.20; N, 3.24; S, 14.01

TABLE 34 Compd. No.. Physical property I-7M-126a ¹H-NMR(CDCl₃) δ0.96(1H, m), 1.23–1.26(2H, m), 1.38–1.46 (6H, m), 1.54–1.63(4H, s),1.97(1H, d, J=3.6Hz), 2.45(1H, m), 3.48–3.53(2H, m), 3.83(3H, s),3.85(1H, m), 4.03(2H, s), 4.12(2H, s), 5.88(1H, d, J=7.8Hz), 6.77(1H, d,J=3.6Hz), 6.86–6.90(2H, m), 7.16(1H, dd, J=4.5, 1.8Hz), 7.21(1H, dd,J=7.8, 1.8Hz), 7.33(1H, d, J=3.6Hz); IR(CHCl₃)3427, 2875, 1639, 1504,1460, 1248, 1221cm⁻¹; [α]_(D) ^(27.0)+36.8±1.5°(c=0.508, MeOH)Anal.(C₂₆H₃₃NO₅S·0.3H₂O)Calcd.(%): C, 65.47; H, 7.10; N, 2.94; S,6.72Found(%): C, 65.30; H, 7.01; N, 3.02; S, 6.54 I-7M-143amp123–125°C.; ¹H-NMR(CDCl₃) δ 1.04(1H, m), 1.20–1.75 (12H, m), 2.01(1H,brs), 2.55(1H, brs), 3.53(2H, dt, J= 1.8, 6.0Hz), 3.98(1H, m),4.02and4.24(2H, s), 6.08(1H, d, J=7.8Hz), 7.17–7.45(7H, m), 7.83(1H, s),8.16(1H, d, J=7.8Hz); IR(Nujol)3280, 2924, 1722, 1612, 1566, 1454, 1242,1228, 1137cm⁻¹; [α]_(D) ²⁶+39.2±0.6°(c=1.012%, MeOH);Anal.(C₂₉H₃₃NO₄S)Calcd.(%)C, 70.85; H, 6.77; N, 2.85; S, 6.52Found(%)C,70.58; H, 6.70; N, 2.94; S, 6.40 I-7M-197a ¹H-NMR(CDCl₃) δ 0.98(1H, m),1.20–1.70(12H, m), 1.98 (1H, d, J=3.3Hz), 2.45(1H, m), 3.23(2H, t,J=8.7Hz), 3.49–3.54(2H, m), 3.86(1H, m), 4.03and4.08(2H, s), 4.58 (2H,t, J=8.7Hz), 5.88(1H, d, J=8.4Hz), 6.20(1H, t, J= 3.6Hz), 6.77–6.82(2H,m), 6.96(1H, d, J=7.2Hz), 7.10 (1H, d, J=7.2Hz), 7.35(1H, d, J=3.6Hz);IR(CHCl₃) 2954, 1732, 1641, 1545, 1506, 1477, 1458, 1254, 1225, 1221,1213, 1207, 1130cm⁻¹; [α]_(D) ²⁶+37.2±0.8°(c=1.008%, MeOH);Anal.(C₂₇H₃₃NO₅S·0.3H₂O)Calcd.(%)C, 66.31; H, 6.93; N, 2.86; S,6.56Found(%)C, 66.24; H, 6.91; N, 2.92; S, 6.52 I-7M-270a mp.141–143°C.;¹H-NMR(CDCl₃) δ 1.02(1H, br), 1.18–1.70 (12H, m), 2.01(1H, brd),2.42(6H, s), 2.48(1H, brs), 3.53 (2H, dt, J=0.9, 6.6Hz), 3.83(1H, m),4.06(2H, s), 5.88 (2H, s), 6.11(1H, d, J=7.8Hz), 7.36(1H, d, J=3.9Hz),7.50(1H, d, J=3.9Hz); IR(Nujol)3327, 3097, 3084, 2555, 1732, 1616, 1556,1234, 1219, 1176, 1134, 1113cm⁻¹; [α]_(D) ²⁶+ 40.5±0.8°(c=1.014,MeOH)Anal.(C₂₄H₃₂N₂O₆S₂) Calcd.(%): C, 56.67; H, 6.37; N, 5.51; S,12.61Found(%): C, 56.56; H, 6.10; N, 5.48; S, 12.38 I-7M-307amp131–132°C.; ¹H-NMR(CDCl₃) δ 0.94(1H, m), 1.20–1.23 (2H, m),1.34–1.39(6H, m), 1.51–1.63(4H, m), 1.94(1H, m), 2.42(1H, m),3.45–3.49(2H, m), 3.81(1H, m), 3.98(3H, s), 4.01(2H, s), 4.59(2H, s),5.85(1H, d, J=7.5Hz), 6.75(1H, d, J=3.3Hz), 7.28–7.36(3H, m,), 7.47(1H,t, J=7.7Hz), 7.79(1H, d, J=3.9Hz), 7.82(1H, d, J=4.8Hz), 7.92(1H, d,J=8.4Hz); IR(Nujol)3340, 3068, 2744, 2546, 1738, 1604, 1560, 1435, 1250,1236, 1146cm⁻¹; [α]_(D) ^(25.5)+36.1±0.8° (c=1.000,MeOH)Anal.(C₃₀H₃₅NO₅S)Calcd.(%): C, 69.07; H, 6.76; N, 2.68; S,6.15Found(%): C, 68.99; H, 6.87; N, 2.74; S, 6.05

TABLE 35 Compd. No.. Physical property I-7M-315a ¹H-NMR(CDCl₃) δ1.04(1H, m), 1.26–1.64(12H, m), 2.03 (1H, m), 2.55(1H, m), 3.54(2H, t,J=5.1Hz), 3.99 (1H, m), 4.03(2H, s), 4.26(2H, s), 6.07–6.10(1H, d,J=7.5Hz), 7.00–7.23(5H, m), 7.43(1H, m), 7.85(1H, s), 8.16(1H, d, J=8.1Hz); IR(CHCl₃)3508, 3437, 2954, 2875, 1780, 1732, 1651, 1518, 1477,1456, 1396, 1363cm⁻¹; [α]_(D) ^(24.0)+38.1±0.8° (c=1.03,MeOH)Anal.(C₂₉H₃₂FNO₄S·0.6MeOH)Calcd.(%): C, 67.22; H, 6.56; N, 2.65;F,3.59; S, 6.06Found(%): C, 67.31; H, 6.57; N, 2.92;F, 3.21; S, 6.09I-7M-316a ¹H-NMR(CDCl₃) δ 1.04(1H, m), 1.23–1.68(11H, m), 2.01 (1H, m),2.55(2H, m), 3.54(2H, t, J=6.6Hz), 3.82(3H, s), 3.99(1H, m), 4.02(2H,s), 4.23(2H, s), 6.09(1H, d, J=8.1Hz), 6.83–6.91(2H, m), 7.05–7.23(3H,m), 7.39(1H, m), 7.85(1H, s), 8.12(1H, d, J=8.1Hz); IR(CHCl₃)3437, 2954,2875, 1780, 1732, 1651, 1601, 1516, 1493, 1464, 1394, 1363, 1246cm⁻¹;[α]_(D) ^(26.0)+35.2±1.5°(c=0.50, MeOH)Anal.(C₃₀H₃₅NO₅S·0.2H₂O)Calcd.(%): C, 68.60; H, 6.79; N, 2.67; S,6.10Found(%): C, 68.56; H, 6.89; N, 2.86; S, 5.93 I-7M-317a¹H-NMR(CDCl₃) δ 1.03(1H, m), 1.22–1.65(11H, m), 2.02 (1H, m), 2.57(1H,m), 3.54(2H, d, J=6.0Hz), 4.00(1H, m), 4.03(3H, s), 4.35(2H, s),6.10(1H, d, J=7.8Hz), 7.08–7.24(4H, m), 7.39–7.44(2H, m), 7.85(1H, s),8.18(1H, d, J=8.4Hz); IR(CHCl₃)3508, 3437, 2954, 2875, 1780, 1732, 1651,1568, 1518, 1495, 1475, 1444, 1394, 1363cm⁻¹; [α]_(D)^(26.0)+34.9±0.8°(c=1.00, MeOH)Anal. (C₂₉H₃₂ClNO₄S)Calcd.(%): C, 66.21;H, 6.13; N, 2.66; Cl, 6.74; S, 6.10Found(%): C, 66.01; H, 6.32; N, 2.89;Cl, 6.03; S, 5.91 I-7M-318a ¹H-NMR(CDCl₃) δ 1.05(1H, m), 1.22–1.64(12H,m), 2.01 (1H, m), 2.56(1H, m), 3.49–3.52(2H, m), 3.97(2H, s), 3.50 (1H,m), 4.24(2H, s), 6.12(1H, d, J=6.3Hz), 6.81–6.91 (2H, m), 7.11–7.18(3H,m), 7.39(1H, m), 7.84(1H, s), 8.12 (1H, d, J=7.8Hz); IR(CHCl₃)3597,3435, 2954, 2875, 1780, 1730, 1649, 1518, 1496, 1456, 1394, 1363,1327cm⁻¹; [α]_(D) ^(27.0)+36.9±0.8° (c=1.01, MeOH)Anal.(C₂₉H₃₃NO₅S·1.2H₂O)Calcd.(%): C, 65.81; H, 6.74; N, 2.65; S,6.06Found(%): C, 65.74; H, 6.59; N, 2.79; S, 5.90 I-7M-327amp137–139°C.; ¹H-NMR(CDCl₃) δ 1.01(1H, m), 1.20–1.70(12H, m), 2.00(1H,d, J=3.0Hz), 2.46(1H, brs), 3.01(2H, t, J=8.7Hz), 3.52(2H, t, J=6.3Hz),3.81(1H, m), 3.98 (2H, t, J=8.4Hz), 4.04(2H, s), 6.11(1H, d, J=7.5Hz),6.98–7.24(3H, m), 7.35(1H, d, J=3.9Hz), 7.46(1H, d, J= 3.9Hz), 7.57(1H,d, J=8.1Hz); IR(Nujol)3325, 2924, 1730, 1616, 1566, 1460, 1444, 1373,1236, 1163, 1138cm⁻¹; [α]_(D) ²⁶+39.2±0.8°(c=1.006%, MeOH); Anal.(C₂₆H₃₂N₂O₆S₂·0.2H₂O)Calcd.(%)C, 58.23; H, 6.09; N, 5.22; S,11.96Found(%)C, 58.19; H, 6.14; N, 5.22; S, 11.85

TABLE 36 Compd. No.. Physical property I-7M-329a mp137–139°C.;¹H-NMR(d₆-DMSO) δ 1.14–1.60(13H, m), 1.91(1H, d, J=3.0Hz), 2.29(1H,brs), 3.05(2H, t, J= 8.4Hz), 3.37(2H, t, J=6.3Hz), 3.57(1H, m), 3.91(2H,s), 4.01(2H, t, J=8.4Hz), 6.91(1H, m), 7.27–7.37(2H, m), 7.78(1H, d,J=3.9Hz), 7.93(1H, d, J=3.9Hz), 8.53 (1H, d, J=6.9Hz); IR(Nujol)3325,2924, 1730, 1618, 1566, 1460, 1444, 1435, 1375, 1234, 1165, 1138,1070cm⁻¹; [α]_(D) ²⁵+38.2±0.8°(c=1.015%, MeOH); Anal.(C₂₆H₃₁FN₂O₆S₂)Calcd.(%)C, 56.71; H, 5.67;F, 3.45; N, 5.09; S,11.65Found(%)C, 56.61; H, 5.47;F, 3.32; N, 5.12; S, 11.54 I-7M-330amp158–160°C.; ¹H-NMR(d₆-DMSO) δ 1.13–1.58(13H, m), 1.91(1H, d, J=3.0Hz),2.29(1H, brs), 2.97(2H, t, J= 8.4Hz), 3.37(2H, t, J=6.9Hz), 3.57(1H, m),3.91(2H, s), 3.97(2H, t, J=8.4Hz), 7.10(1H, d, J=8.7Hz), 7.43 (1H, dd,J=4.5, 8.4Hz), 7.72(1H, d, J=3.9Hz), 7.92 (1H, d, J=3.9Hz), 8.52(1H, d,J=6.9Hz); IR(Nujol) 3325, 3095, 2924, 1732, 1618, 1566, 1481, 1460,1444, 1373, 1236, 1221, 1167, 1140, 1038cm⁻¹; [α]_(D) ²⁵⁺38.2±0.8°(c=1.009%, MeOH); Anal.(C₂₆H₃₁FN₂O₆S₂) Calcd.(%)C, 56.71; H,5.67;F, 3.45; N, 5.09; S, 11.65 Found(%)C, 56.51; H, 5.74;F, 3.30; N,5.09; S, 11.57 I-7M-331a mp152–154°C.; ¹H-NMR(d₆-DMSO) δ 1.14–1.60(13H,m), 1.92(1H, d, J=2.7Hz), 2.29(1H, brs), 2.98(2H, t, J= 8.4Hz), 3.37(2H,t, J=6.6Hz), 3.58(1H, m), 3.91(2H, s), 3.99(2H, t, J=8.4Hz), 6.88(1H,ddd, J=2.4, 8.1, 9.0Hz), 7.16–7.26(2H, m), 7.82(1H, d, J=4.2Hz),7.94(1H, d, J=4.2Hz), 8.54(1H, d, J=7.5Hz); IR(Nujol)3317, 3091, 2924,1734, 1616, 1568, 1491, 1460, 1446, 1435, 1371, 1261, 1234, 1221, 1176,1163, 1142, 1092, 1036cm⁻¹; [α]_(D) ²⁵+38.7±0.8°(c=1.012%, MeOH); Anal.(C₂₆H₃₁FN₂O₆S₂)Calcd.(%)C, 56.71; H, 5.67; F, 3.45; N, 5.09; S,11.65Found(%)C, 56.49; H, 5.36;F, 3.34; N, 5.10; S, 11.27 I-7M-332amp100–103°C.; ¹H-NMR(CDCl₃) δ 1.01(1H, m), 1.20–1.82(14H, m), 2.01(1H,d, J=3.3Hz), 2.47(1H, brs), 2.53(2H, t, J=6.6Hz), 3.53(2H, t, J=6.3Hz),3.79–3.88 (3H, m), 4.05(2H, s), 6.07(1H, d, J=7.8Hz), 7.03–7.23(4H, m),7.32(1H, d, J=3.9Hz), 7.78(1H, dd, J=0.9, 8.1Hz); IR(Nujol)3329, 2925,1730, 1614, 1562, 1458, 1363, 1346, 1234, 1159cm⁻¹; [α]_(D) ²⁴+37.7±0.8°(c=1.018%, MeOH); Anal.(C₂₇H₃₄N₂O₆S₂·0.4H₂O) Calcd.(%)C, 58.55; H, 6.33;N, 5.06; S, 11.58Found(%) C, 58.84; H, 6.41; N, 5.02; S, 11.30

TABLE 37 Compd. No.. Physical property I-7M-333a mp 125–128° C.;¹H-NMR(CDCl₃) δ 1.01(1H, m), 1.20– 1.75(12H, m), 2.01(1H, d, J=3.0Hz),2.47(1H, brs), 3.53(2H, t, J=6.0Hz), 3.79–3.96(5H, m), 4.05(2H, s),6.06(1H, d, J=7.8Hz), 6.85(1H, dd, J=1.5, 8.1Hz), 6.96(1H, m), 7.11(1H,m), 7.29(1H, d, J=4.2Hz), 7.34 (1H, d, J=4.2Hz), 7.83(1H, dd, J=1.5,8.1Hz); IR (Nujol) 3325, 3084, 2924, 1730, 1612, 1562, 1491, 1460, 1369,1250, 1236, 1165, 1138cm⁻¹; [α]_(D) ^(26+36.4±0.8°) (c=1.008%, MeOH);Anal.(C₂₆H₃₂N₂O₇S₂.0.3H₂O) Calcd.(%) C, 56.36; H, 5.93; N, 5.06; S,11.57 Found(%) C, 56.36; H, 5.72; N, 5.08; S, 11.53 I-7M-334a mp127–129° C.; ¹H-NMR(CDCl₃) δ 1.02(1H, m), 1.20– 1.70(12H, m), 2.01(1H,d, J=3.3Hz), 2.48(1H, brs), 3.05(2H, dd, J=5.7, 9.0Hz), 3.53(2H, t,J=6.3Hz), 3.82(1H, m), 4.03–4.07(4H, m), 6.08(1H, d, J=8.1Hz),7.07–7.33(5H, m), 7.67(1H, m); IR(Nujol) 3315, 2924, 1761, 1728, 1616,1550, 1467, 1363, 1165cm⁻¹; [α]_(D) ²⁴+37.1±0.8°(c=1.010%, MeOH); Anal.(C₂₆H₃₂N₂O₆S₃.0.1Hexane) Calcd.(%) C, 55.72; H, 5.87; N, 4.89; S, 16.78Found(%) C, 55.86; H, 5.94; N, 4.84; S, 16.61 I-7M-336a mp 209–212° C.;¹H-NMR(d₆-DMSO) δ 1.11–1.56(13H, m), 1.91(1H, m), 2.29(1H, brs),3.37(2H, t, J=6.3Hz), 3.58(1H, m), 3.91(2H, s), 4.63(4H, s),7.20–7.35(4H, m), 7.77(1H, d, J=3.9Hz), 7.96(1H, d, J=3.9Hz), 8.51 (1H,d, J=7.5Hz); IR(Nujol) 3332, 2924, 1736, 1616, 1562, 1468, 1354, 1240,1165, 1140, 1092cm⁻¹; Anal. (C₂₆H₃₂N₂O₆S₂) Calcd.(%) C, 58.62; H, 6.06;N, 5.26; S, 12.04 Found(%) C, 58.38; H, 5.98; N, 5.25; S, 11.82I-7M-337a ¹H-NMR(CDCl₃) δ 1.04(1H, m), 1.23–1.32(3H, m), 1.43–1.69(8H,s), 2.02(1H, m), 2.52–2.54(2H, m), 3.53 (2H, t, J=6.3Hz), 4.01(1H, m),4.03(2H, s), 4.28(2H, s), 6.06(1H, d, J=8.1Hz), 7.01–7.07(2H, m),7.15–7.31 (4H, m), 7.65(1H, dd, J=7.5, 0.9Hz), 8.17(1H, s); IR (CHCl₃)3323, 2656, 2548, 1728, 1621, 1562, 1456, 1234, 1130cm⁻¹; [α]_(D)^(27.0)+26.7±0.7°(c=1.001, MeOH) Anal. (C₂₉H₃₂FNO₅.0.5H₂O) Calcd.(%): C,69.31; H, 6.62; N, 2.79; F, 3.58 Found(%): C, 69.19; H, 6.67; N, 2.82;F, 3.28 I-7M-342a ¹H-NMR(CDCl₃) δ 1.05(1H, m), 1.22–1.63(12H, m), 2.01(1H, m), 2.55(1H, m), 3.49–3.53(2H, m), 3.99(1H, m), 4.01(2H, s),6.14(1H, br), 7.18–7.26(5H, m), 7.43–7.54 (2H, m), 7.85(1H, s), 8.32(1H,d, J=7.8Hz); IR(CHCl₃) 3438, 2954, 2875, 1780, 1730, 1649, 1583, 1516,1477, 1456, 1375cm⁻¹; [α]_(D) ^(26.0)+38.5±0.8°(c=1.03, MeOH)

TABLE 38 Compd. No.. Physical property I-7M-343a ¹H-NMR(CDCl₃) δ1.05(1H, m), 1.24–1.63(12H, m), 2.05 (1H, m), 2.54(1H, m), 3.54(2H, t,J=8.1Hz), 3.94(1H, m), 4.03(2H, s), 6.17(1H, d, J=7.5Hz), 7.45–7.63(4H,m), 7.94(1H, s), 8.01–8.11(3H, m), 8.62(1H, d, J=8.4Hz); IR(CHCl₃) 3437,3375, 2954, 2875, 1780, 1730, 1518, 1383, 1315, 1309cm⁻¹; [α]_(D)^(25.0)+33.3±0.7°(c=1.04, MeOH) I-7M-385a ¹H-NMR(CDCl₃) δ 1.07(1H, m),1.20–1.72(12H, m), 2.04 (1H, m), 2.56(1H, m), 3.52(2H, dt, J=6.3,1.8Hz), 3.97 (1H, s), 4.03(2H, s), 6.27(2H, t, J=2.4Hz), 6.42(1H, d,J=7.2Hz), 7.21(2H, t, J=2.4Hz), 7.56(1H, t, J=7.8Hz), 7.68(1H, d,J=7.8Hz), 8.38(1H, dd, J=7.8, 1.2Hz), 8.43(1H, s); IR(CHCl₃) 3450, 3103,3022, 2954, 2875, 1732, 1651, 1518, 1456, 1373, 1221, 1188, 1163,1057cm⁻¹; [α]_(D) ^(22.0)+39.9±0.8°(c=1.006, MeOH) Anal.(C₂₆H₃₀N₂O₆S₂.0.1H₂O) Calcd.(%): C, 58.65; H, 5.72; N, 5.26; S, 12.04Found(%): C, 58.40; H, 5.82; N, 5.08; S, 11.88 I-7M-389a mp 94–96° C.;¹H-NMR(CDCl₃) δ 0.99(1H, m), 1.21–1.27 (2H, m), 1.38–1.46(6H, m),1.55–1.68(4H, m), 1.99(1H, m), 2.23(3H, s), 2.46(1H, m), 3.21(2H, t,J=8.7Hz), 3.46–3.57(2H, m), 3.83(1H, m), 4.05(2H, s), 4.62(2H, t,J=8.7Hz), 5.95(1H, d, J=7.8Hz), 6.90(1H, s), 6.96 (1H, s), 7.07(1H, d,J=3.9Hz), 7.37(1H, d, J=3.9Hz); IR(Nujol) 3327, 3074, 2750, 2650, 2613,2551, 1728, 1604, 1562, 1234, 1223, 1136cm⁻¹; [α]_(D) ²³+35.5±0.7°(c=1.014, MeOH) Anal.(C₂₇H₃₃NO₅S₂) Calcd.(%): C, 62.88; H, 6.45; N,2.72; S, 12.44 Found(%): C, 62.96; H, 6.46; N, 2.68; S, 12.33 I-7M-390amp 99–101° C.; ¹H-NMR(CDCl₃) δ 0.99(1H, m), 1.20– 1.27(2H, m),1.37–1.45(6H, m), 1.54–1.63(4H, m), 1.98 (1H, m), 2.39(3H, s), 2.46(1H,m), 3.46–3.56(2H, m), 3.83 (1H, m), 4.04(2H, s), 5.95(1H, d, J=7.8Hz),6.72(1H, d, J=2.1Hz), 7.09(1H, m), 7.18(1H, d, J=3.9Hz), 7.33 (1H, m),7.39(1H, d, J=3.9Hz), 7.63(1H, d, J=2.1Hz); IR(CHCl₃) 3508, 3444, 3425,2667, 2567, 1780, 1732, 1645, 1531, 1500, 1421, 1321, 1130cm⁻¹; [α]_(D)²⁴+36.1±0.8°(c=1.008, MeOH) Anal. (C₂₇H₃₁NO₅S₂.0.2H₂O) Calcd.(%): C,62.69; H, 6.12; N, 2.71; S, 12.40 Found(%): C, 62.54; H, 5.98; N, 2.68;S, 12.55

TABLE 39 Compd. No.. Physical property I-7M-391a ¹H-NMR(CDCl₃) δ1.06(1H, m), 1.24–1.29(2H, m), 1.38–1.47 (6H, m), 1.55–1.59(4H, m),2.00(1H, m), 2.32(3H, s), 2.48(1H, m), 3.19(2H, t, J=8.7Hz), 3.52(2H, t,J=6.3Hz), 3.83(1H, m), 4.05(2H, s), 4.72(2H, t, J=8.7Hz), 6.26(1H, d,J=7.8Hz), 7.22(1H, s), 7.43(1H, d, J=3.9Hz), 7.50(1H, s), 7.70(1H, d,J=3.9Hz); IR(CHCl₃) 3508, 3440, 3423, 3377, 2567, 2463, 1778, 1732,1653, 1529, 1504, 1481, 1327, 1151cm⁻¹; [α]_(D) ²⁵+40.6±0.8°(c=1.004,MeOH) Anal. (C₂₇H₃₃NO₇S₂.0.5H₂O) Calcd.(%): C, 58.25; H, 6.16; N, 2.52;S, 11.52 Found(%): C, 58.18; H, 6.07; N, 2.45; S, 11.55 I-7M-392a mp136–140° C.; ¹H-NMR(CDCl₃+CD₃OD) δ 1.09(1H, m), 1.22–1.29(2H, m),1.33–1.43(5H, m), 1.52–1.58(4H, m), 1.96 (1H, m), 2.48–2.51(2H,m)+2.51(3H, s), 3.42–3.53(2H, m), 3.75(1H, m), 4.01(2H, s), 6.68(1H, d,J=7.2Hz), 6.78(1H, d, J=2.1Hz), 7.48(1H, d, J=3.9Hz), 7.64(1H, s),7.74(1H, d, J=2.1Hz), 7.76(1H, s), 7.82(1H, d, J=3.9Hz); IR (Nujol)3280, 3141, 3114, 3084, 2750, 2650, 2548, 1732, 1618, 1566, 1460, 1323,1223, 1153, 1126cm⁻¹; [α]_(D) ²⁵+ 40.5±0.8°(c=1.004, MeOH)Anal.(C₂₇H₃₁NO₇S₂.0.2H₂O) Calcd.(%): C, 59.04; H, 5.76; N, 2.55; S,11.68 Found(%): C, 59.01; H, 5.77; N, 2.51; S, 11.50 I-7M-393a mp104–107° C.; ¹H-NMR(CDCl₃) δ 0.90(3H, t, J=7.4Hz), 0.98(1H, m),1.21–1.64(16H, m), 1.99(1H, m), 2.46–2.51(3H, m), 3.23(2H, t, J=8.7Hz),3.49–3.55(2H, m), 3.84(1H, m), 4.05(2H, s), 4.62(2H, t, J=8.7Hz),5.92(1H, d, J=7.8Hz), 6.93(1H, s), 6.98(1H, s), 7.07(1H, d, J=3.6Hz),7.36(1H, d, J=3.6Hz); IR(CHCl₃) 3444, 3425, 2569, 1780, 1732, 1643,1531, 1498, 1479, 1464, 1419, 1317, 1132cm⁻¹; [α]_(D) ²⁴+33.3±0.7°(c=1.009, MeOH) Anal.(C₃₀H₃₉NO₅S₂.0.2H₂O) Calcd.(%): C, 64.19;H, 7.07; N, 2.50; S, 11.42 Found(%): C, 64.09; H, 6.95; N, 2.55; S,11.36 I-7M-396a ¹H-NMR(CDCl₃) δ 1.06(1H, m), 1.26–1.69(12H, m), 2.03(1H, m), 2.56(1H, m), 3.55(2H, t, J=5.1Hz), 4.00(1H, m), 4.04(2H, s),6.11(1H, d, J=8.1Hz), 6.88(1H, d, J=7.5Hz), 7.07–7.19(3H, m),7.34–7.42(3H, m), 7.89(1H, s), 8.03(1H, d, J=8.1Hz); IR(KBr) 3383, 3076,2949, 2929, 2868, 2520, 1736, 1604, 1550, 1487, 1466, 1390, 1298, 1281,1248, 1213, 1134cm⁻¹; [α]_(D) ^(25.0)+35.4±3.0°(c=0.26, MeOH) Anal.(C₂₈H₃₁NO₅S.0.5H₂O) Calcd.(%): C, 66.91; H, 6.42; N, 2.79; S, 6.38Found(%): C, 66.98; H, 6.35; N, 2.85; S, 6.29 I-7M-412a ¹H-NMR(CDCl₃) δ1.05(1H, m), 1.22–1.70(12H, m), 2.01 (1H, d, J=3.3Hz), 2.50(1H, brs),3.53(2H, t, J=6.3Hz), 3.92(1H, m), 4.05(2H, s), 6.11(1H, d, J=7.8Hz),7.27–7.62 (6H, m), 7.79(1H, d, J=1.8Hz); IR(CHCl₃) 3444, 2954, 1780,1732, 1649, 1547, 1514, 1491, 1219, 1213, 1128cm⁻¹; [α]_(D)²⁴+49.9±0.9°(c=1.008%, MeOH); Anal. (C₂₄H₂₉NO₄S.0.3H₂O) Calcd.(%) C,66.58; H, 6.89; N, 3.24; S, 7.41Found(%) C, 66.73; H, 6.90; N, 3.35 S,7.29

TABLE 40 Compd. No.. Physical property I-7M-424a ¹H-NMR(CDCl₃) δ1.00(1H, m), 1.22–1.64(12H, m), 1.98 (1H, m), 2.55(1H, m), 3.48(2H, t,J=6.9Hz), 3.94(1H, m), 3.99(2H, s), 4.15(2H, s), 6.13(1H, d, J=8.1Hz),6.84(1H, d, J=2.1Hz), 7.20–7.30(5H, m), 7.74(1H, s), 7.79(1H, d,J=2.1Hz); IR(KBr) 3433, 3246, 3024, 2954, 2875, 1730, 1639, 1599, 1518,1495, 1475, 1454, 1421, 1352cm⁻¹; [α]_(D) ^(26.0)+34.0±0.7°(c=1.00,MeOH) Anal.(C₂₉H₃₃NO₅S.0.6H₂O) Calcd.(%): C, 67.18; H, 6.65; N, 2.70; S,6.18 Found(%): C, 67.21; H, 6.66; N, 2.71; S, 5.99 I-7M-446a¹H-NMR(CDCl₃) δ 1.00(1H, m), 1.22–1.64(12H, m), 1.98(1H, m), 2.55(1H,m), 3.47(2H, t, J=6.3Hz), 3.96 (1H, m), 3.98(2H, s), 4.17(2H, s),6.16(1H, d, J=8.1Hz), 6.82(1H, d, J=2.4Hz), 6.99–7.22(4H, m), 7.76(1H,s), 7.82(1H, d, J=2.4Hz); IR(CHCl₃) 3593, 3433, 3244, 2954, 2875, 1728,1639, 1599, 1518, 1491, 1456, 1421, 1362cm⁻¹; [α]_(D)^(22.0)+31.2±0.7°(c=1.01, MeOH) Anal. (C₂₉H₃₂FNO₅S.0.9H₂O) Calcd.(%): C,64.28; H, 6.29; N, 2.58; F, 3.51; S, 5.92 Found(%): C, 64.39; H, 6.29;N, 2.52; F, 3.40; S, 5.72 I-7M-447a ¹H-NMR(CDCl₃) δ 1.04(1H, m),1.22–1.69(12H, m), 2.03 (1H, m), 2.55(1H, m), 3.55(2H, t, J=6.6Hz),3.96(1H, m), 4.04(2H, s), 6.08(1H, d, J=7.8Hz), 7.16(1H, dd, J= 8.7 and2.7Hz), 7.25–7.35(5H, m), 7.88(1H, s), 8.03 (1H, dd, J=9.6 and 2.7Hz);IR(CHCl₃) 3510, 3438, 2954, 2875, 1780, 1732, 1655, 1591, 1558, 1514,1477, 1441, 1383cm⁻¹; [α]_(D) ^(24.0)+38.1±0.8°(c=1.01, MeOH)Anal.(C₂₈H₃₀FNO₄S₂.0.9H₂O) Calcd.(%): C, 61.83; H, 5.89; N, 2.58; F,3.49; S, 11.79 Found(%): C, 61.91; H, 5.73; N, 2.65; F, 3.56; S, 11.67I-7M-448a ¹H-NMR(CDCl₃) δ 1.05(1H, m), 1.22–1.63(12H, m), 2.00 (1H, m),2.53(1H, m), 3.54(2H, m), 3.90(1H, m), 4.04 (2H, s), 6.19(1H, d,J=7.8Hz), 7.47–7.83(3H, m), 7.85 (1H, dd, J=7.8 and 2.4Hz),8.00–8.05(3H, m), 8.38(1H, dd, J=9.3 and 2.4Hz); IR(CHCl₃) 3437, 3386,2954, 2875, 1780, 1730, 1655, 1601, 1518, 1477, 1446, 1396, 1325,1309cm⁻¹; [α]_(D) ^(24.0)+31.5±0.7°(c=1.01, MeOH)Anal.(C₂₈H₃₀FN₆S₂.0.9H₂O) Calcd.(%): C, 58.40; H, 5.57; N, 2.43; F,3.30; S, 11.14 Found(%): C, 58.43; H, 5.54; N, 2.38; F, 3.16; S, 10.78I-7N-1a ¹H-NMR(CDCl₃) δ 1.10–1.70(7H, m), 2.00–2.32(3H, m), 2.51(1H, m),3.83(1H, m), 4.07–4.21(4H, m), 5.54–5.70 (2H, m), 6.26(1H, d, J=7.5Hz),6.32–6.35(2H, m), 7.15–7.18(2H, m), 7.38(1H, d, J=4.2Hz), 7.57(1H, d, J=4.2Hz); IR(CHCl₃) 3440, 1732, 1655, 1531, 1506, 1456, 1383, 1192, 1167,1057, 1034cm⁻¹; [α]_(D) ²⁴+67.3±1.1°(c=1.005, MeOH) Anal.(C₂₂H₂₆N₂O₆S₂.0.3H₂O) Calcd.(%): C, 54.60; H, 5.54; N, 5.79; S, 13.25Found(%): C, 54.58; H, 5.50; N, 5.65; S, 13.15

TABLE 41 No. fo Compd. Physical property I-7N-1b ¹H-NMR(CDCl₃) δ1.16–1.70(7H, m), 2.04(1H, m), 2.12–2.18(2H, m), 2.56(1H, brs), 3.72(3H,s), 3.78(1H, m), 4.05–4.16(4H, m), 5.57–5.76(2H, m), 6.32–6.34(2H, m),6.39(1H, d, J=6.6Hz), 7.15–7.17(2H, m), 7.40(1H, d, J= 3.9Hz), 7.56(1H,d, J=3.9Hz) I-7P-1a ¹H-NMR(CD₃OD) δ 1.28–1.64(8H, m), 2.02–2.13(3H, m),2.47(1H, m), 3.71(1H, m), 3.98(2H, s), 4.25(2H, d, J= 22.2Hz), 5.30(1H,dt, J=8.4 and 22.2Hz), 6.36(2H, m), 7.23(2H, m), 7.70(1H, d, J=3.9Hz),7.75(1H, d, J=3.9Hz); IR(CHCl₃) 3419, 2956, 1635, 1604, 1537, 1508,1456, 1431, 1381, 1167, 1076, 1057, 1036cm⁻¹; [α]_(D) ²⁵+45.7±0.8°(c=1.02, MeOH) I-7P-1e ¹H-NMR(CDCl₃) δ 1.10–1.72(7H, m), 2.06–2.26(3H,m), 2.51(1H, m), 3.29(3H, s), 3.84(1H, m), 4.01–4.31(4H, m), 5.36(1H,dt, J=9.0 and 20.7Hz), 6.15(1H, d, J=6.6Hz), 6.34(2H, m), 7.16(2H, m),7.38(1H, d, J=4.2Hz), 7.58 (1H, d, J=4.2Hz), 9.26(1H, s); IR(CHCl₃)3442, 3352, 2956, 2829, 1728, 1655, 1531, 1506, 1456, 1452, 1402, 1383,1348, 1167, 1109, 1057, 1034cm⁻¹; [α]_(D) ²⁵+51.8±0.9° (c=1.03, MeOH)Anal.(C₂₃H₂₈FN₃O₇S₃0.5MeOH) Calcd.(%): C, 47.86; H, 5.13; N, 7.13; F,3.22; S, 16.31 Found(%): C, 48.09; H, 5.02; N, 7.38; F, 3.12; S, 16.12I-7R-1a ¹H-NMR(CDCl₃) δ 1.02(1H, m), 1.23–1.72(12H, m), 2.02 (1H, d,J=3.9Hz), 2.48(1H, brs), 2.63(2H, t, J=7.2Hz), 3.21(2H, s), 3.83(1H, m),6.17(1H, d, J=7.5Hz), 6.32–6.35 (2H, m), 7.15–7.17(2H, m), 7.37(1H, d,J=3.9Hz), 7.57(1H, d, J=3.9Hz); IR(Nujol) 3348, 2924, 1711, 1641, 1622,1550, 1541, 1456, 1375, 1290, 1190, 1167, 1057cm⁻¹; [α]_(D)^(25+42.8±0.8°(c=1.005%, MeOH); Anal.) (C₂₂H₂₈N₂O₅S₃) Calcd.(%) C,53.20; H, 5.68; N, 5.64; S, 19.37 Found(%) C, 53.41; H, 5.58; N, 5.54;S, 19.08 I-7R-88a ¹H-NMR(CDCl₃) δ 0.99(1H, m), 1.21–1.72(12H, m), 1.98(1H, d, J=3.9Hz), 2.47(1H, brs), 2.64(2H, t, J=7.2Hz), 3.20(2H, s),3.87(1H, m), 4.16(2H, s), 5.96(1H, d, J=7.5Hz), 6.79(1H, d, J=3.6Hz),6.96(1H, d, J=4.8Hz), 7.06 (1H, d, J=2.1Hz), 7.26–7.30(2H, m), 7.37(1H,d, J=3.9Hz); IR(CHCl₃) 2877, 1711, 1641, 1545, 1508, 1458, 1298, 1282,1225, 1205cm⁻¹; [α]_(D) ^(25+42.8±0.8°(c=1.005%,) MeOH);Anal.(C₂₃H₂₉NO₃S₃.0.2H₂O) Calcd.(%) C, 59.12; H, 6.34; N, 3.00; S, 20.59Found(%) C, 59.18; H, 6.01; N, 3.04; S, 20.28 I-7R-270a ¹H-NMR(CDCl₃) δ1.03(1H, br), 1.18–1.70(12H, m), 2.01 (1H, brd), 2.41(6H, s), 2.46(1H,brs), 2.62(2H, t, J=7.2Hz), 3.21(2H, s), 3.82(1H, m), 5.88(2H, s),6.23(1H, d, J= 7.2Hz), 7.36(1H, d, J=3.9Hz), 7.49(1H, d, J=3.9Hz);IR(CHCl₃) 3508, 3442, 2673, 1709, 1657, 1531, 1504, 1375, 1180,1119cm⁻¹; [α]_(D) ²⁶+39.2±0.8°(c=1.010, MeOH) Anal.(C₂₄H₃₂N₂O₅S₃.0.3H₂O) Calcd.(%): C, 54.94; H, 6.15; N, 5.34; S, 18.33Found(%): C, 54.44; H, 6.04; N, 5.28; S, 18.08

TABLE 42 Compd. No.. Physical property I-7R-307a ¹H-NMR(CDCl₃) δ0.93(1H, m), 1.17–1.22(2H, m), 1.34–1.41(6H, m), 1.52–1.58(4H, m),1.94(1H, m), 2.43(1H, m), 2.59 (2H, t, J=7.2Hz), 3.16(2H, s), 3.79(1H,m), 3.97(3H, s), 4.59(2H, s), 5.90(1H, d, J=7.8Hz), 6.74(1H, d,J=3.9Hz), 7.29(1H, d, J=3.9Hz), 7.29–7.36(2H, m,), 7.46(1H, m),7.78–7.83(2H, m), 7.92(1H, d, J=8.4Hz); IR(CHCl₃) 3446, 3425, 3062,2877, 2673, 1711, 1639, 1597, 1542, 1512, 1265, 1254cm⁻¹; [α]_(D)^(25.5)+35.8±0.8°(c=1.007, MeOH) Anal. (C₃₀H₃₅NO₄S₂.0.2H₂O) Calcd.(%):C, 66.56; H, 6.59; N, 2.59; S, 11.85 Found(%): C, 66.53; H, 6.70; N,2.65; S, 11.78 I-8B-1a ¹H-NMR(CDCl₃) δ 1.06(1H, m), 1.19–1.30(2H, m),1.34–1.44 (4H, m), 1.54–1.68(4H, m), 2.04–2.12(5H, m), 2.35(2H, t, J=7.5Hz), 2.51(1H, brs), 3.82(1H, m), 5.29–5.42(2H, m), 6.21 (1H, d,J=6.9Hz), 6.32–6.34(2H, m), 7.15–7.17(2H, m), 7.35 and 7.56(each 1H,each d, each J=3.9Hz); IR(CHCl₃) 3512, 3442, 2679, 1707, 1657, 1529,1504, 1456, 1383, 1192, 1167, 1057, 1034cm⁻¹; [α]_(D)²⁴+69.7±1.1°(c=1.004, MeOH) Anal. (C₂₄H₃₀N₂O₅S₂.0.2H₂O) Calcd.(%): C,58.32; H, 6.20; N, 5.67; S, 12.98 Found(%): C, 58.30; H, 6.07; N, 5.67;S, 12.84 I-8C-1a ¹H-NMR(CDCl₃) δ 1.01(1H, m), 1.25–1.45(10H, m),1.53–1.66 (4H, m), 2.00(1H, m), 2.48(1H, m), 3.52(2H, t, J=7.1Hz),3.80(1H, m), 4.08(2H, s), 6.22(1H, d, J=7.5Hz), 6.33–6.34(2H, m),7.15–7.17(2H, m), 7.38(1H, d, J=3.9Hz), 7.57(1H, d, J=3.9Hz); IR(CHCl₃)3440, 3145, 2578, 1780, 1730, 1657, 1529, 1383, 1192, 1167, 1057cm⁻¹;[α]_(D) ^(25.0)+ 45.0±0.8°(c=1.010, MeOH) Anal.(C₂₃H₃₀N₂O₆S₂.0.4H₂O)Calcd.(%): C, 55.05; H, 6.19; N, 5.58; S, 12.78 Found(%): C, 55.09; H,6.08; N, 5.61; S, 12.74 I-8C-88a ¹H-NMR(CDCl₃) δ 0.97(1H, m),1.23–1.47(10H, m), 1.55–1.61 (4H, m), 1.97(1H, m), 2.48(1H, m), 3.52(2H,t, J=6.6Hz), 3.83(1H, m), 4.06(2H, s), 4.16(2H, s), 5.93(1H, d, J=7.8Hz), 6.79(1H, dt, J=3.9, 0.9Hz), 6.96(1H, dd, J=5.1, 1.2Hz), 7.06(1H,m), 7.29(1H, dd, J=5.1, 3.0Hz), 7.37(1H, d, J= 3.9Hz); IR(CHCl₃) 3444,3427, 3107, 3022, 2954, 2875, 1780, 1732, 1643, 1545, 1506, 1221, 1211,1128cm⁻¹; [α]_(D) ^(25.0)+ 39.6±0.8°(c=1.016, MeOH)Anal.(C₂₄H₃₁NO₄S₂.0.3H₂O) Calcd.(%): C, 61.72; H, 6.82; N, 3.00; S,13.73 Found(%): C, 61.79; H, 6.69; N, 3.11; S, 13.59 I-9B-1a¹H-NMR(CDCl₃) δ 1.06(1H, m), 1.22–1.45(8H, m), 1.59–1.67 (4H, m),2.03–2.13(5H, m), 2.33(2H, t, J=7.5Hz), 2.52(1H, brs), 3.82(1H, m),5.26–5.42(2H, m), 6.18(1H, d, J=7.2Hz), 6.33–6.34(2H, m), 7.15–7.17(2H,m), 7.36 and 7.57(each 1H, each d, each J=3.9Hz); IR(CHCl₃) 3514, 3442,2677, 1709, 1657, 1529, 1504, 1456, 1383, 1192, 1167, 1057, 1034cm⁻¹;[α]_(D) ^(24.5)+72.2±1.1°(c=1.006, MeOH) Anal.(C₂₅H₃₂N₂O₅S₂) Calcd.(%):C, 59.50; H, 6.39; N, 5.55; S, 12.71 Found(%): C, 59.24; H, 6.48; N,5.60; S, 12.46

TABLE 43 Compd. No.. Physical property II-4A-55a ¹H-NMR(CDCl₃) δ0.90(1H, d, J=10.2Hz), 1.09 and 1.22(3H, s), 1.40–2.40(12H, m), 2.38(3H,s), 4.17(1H, m), 4.56(1H, brs), 5.98(1H, m), 6.19(1H, t, J=3.0Hz),6.24(1H, d, J=8.7Hz), 7.17(1H, dd, J=1.5, 3.3Hz), 7.31(1H, d, J=3.9Hz),7.51(1H, d, J=3.9Hz); IR (CHCl₃) 3446, 1709, 1657, 1529, 1504, 1375,1182, 1161, 1144, 1053cm⁻¹; [α]_(D) ²³+28.9±0.7°(c=1.011, MeOH)Anal.(C₂₃H₃₀N₂O₅S₂.0.4H₂O) Calcd.(%): C, 56.86 H, 6.39; N, 5.77; S,13.20 Found(%): C, 57.24; H, 6.36; N, 5.73; S, 12.72. II-4B-55a¹H-NMR(CDCl₃) δ 0.90(1H, d, J=10.5Hz), 1.10(3H, s), 1.23(3H, s),1.43–2.35(10H, m), 2.38(3H, s), 4.20(1H, m), 4.96(1H, dt, J=11.4 and49.2Hz), 5.98(1H, m), 6.19–6.21(2H, m), 7.17(1H, m), 7.29(1H, d,J=3.9Hz), 7.51(1H, d, J=3.9Hz); IR(CHCl₃) 3446, 2925, 2870, 1730, 1657,1529, 1504, 1471, 1375, 1159, 1144, 1053, 1022cm⁻¹; [α]_(D)²⁴+24.6±0.6°(c=1.04, MeOH) Anal. (C₂₃H₂₉FN₂O₅S₂.0.6MeOH) Calcd.(%): C,54.95; H, 6.14; N, 5.43; F, 3.68; S, 12.43 Found(%): C, 54.94; H, 5.97;N, 5.65; F, 3.55; S, 12.24 II-4C-55a ¹H-NMR(CDCl₃) δ 0.92(1H, d,J=10.5Hz), 1.10 and 1.24(3H, s), 1.56(1H, ddd, J=2.7, 5.7, 12.0Hz),1.96–2.70 (8H, m), 2.37(3H, s), 4.25(1H, m), 5.88(1H, brd, J= 15.9Hz),5.99(1H, m), 6.17–6.21(2H, m), 7.03(1H, dt, J=7.2, 15.9Hz), 7.17(1H, dd,J=1.5, 3.3Hz), 7.27(1H, d, J=3.9Hz), 7.47(1H, d, J=3.9Hz); IR(CHCl₃)3446, 1697, 1655, 1529, 1504, 1375, 1182, 1161, 1144, 1053cm⁻¹; [α]_(D)²³+5.4±0.5°(c=1.002, MeOH) Anal. (C₂₃H₂₈N₂O₅S₂.0.4H₂O) Calcd.(%):C,57.10; H, 6.00; N, 5.79; S, 13.26 Found(%): C, 57.14; H, 5.89; N, 5.78;S, 13.01. II-4D-55a ¹H-NMR(CDCl₃) δ 0.97(1H, d, J=10.5Hz), 1.09 and1.23(3H, s), 1.60(1H, ddd, J=2.7, 5.7, 10.8Hz), 1.96–2.40 (6H, m),2.39(3H, s), 2.72–3.01(2H, m), 4.25(1H, m), 5.85(1H, brd, J=11.7Hz),5.98(1H, m), 6.17–6.21 (2H, m), 6.40(1H, dt, J=7.8, 11.7Hz), 7.18(1H,dd, J= 1.8, 3.3Hz), 7.32(1H, d, J=4.2Hz), 7.54(1H, d, J=4.2Hz);IR(CHCl₃) 3519, 3446, 1697, 1658, 1529, 1504, 1375, 1182, 1161, 1144,1053cm⁻¹; [α]_(D) ²³+63.6±1.0° (c=1.006, MeOH)Anal.(C₂₃H₃₂₈N₂O₅S₂.0.3H₂O) Calcd.(%): C, 57.31; H, 5.98; N, 5.81; S,13.30 Found(%): C, 57.48; H, 5.93; N, 5.75; S, 12.90

TABLE 44 Compd. No.. Physical property II-4F-55a ¹H-NMR(CDCl₃) δ0.94(1H, d, J=10.5Hz), 1.09(3H, s), 1.24(3H, s), 1.59(1H, m),2.03–2.34(5H, m), 2.39(3H, s), 2.62(1H, m), 2.92(1H, m), 4.26(1H, m),5.99(1H, m), 6.06(1H, dt, J=8.4 and 21.0Hz), 6.20(1H, m), 7.18 (1H, m),7.28(1H, m), 7.33(1H, d, J=3.9Hz), 7.53(1H, d, J=3.9Hz); IR(CHCl₃)33446, 2925, 2870, 1711, 1658, 1529, 1504, 1442, 1375, 1161, 1070, 1053,1018cm⁻¹; [α]_(D) ²⁵+52.9±0.9°(c=1.02, MeOH) Anal.(C₂₃H₂₇FN₂O₅S₂.0.8MeOH) Calcd.(%): C, 54.95; H, 5.85; N, 5.38; F, 3.65;S, 12.33 Found(%): C, 54.72; H, 5.61; N, 5.67; F, 3.43; S, 12.16II-5A-1a ¹H-NMR(CDCl³) δ 0.91(1H, d, J=10.5Hz), 1.08(3H, s), 1.22(3H,s), 1.33–2.38(14H, m), 4.18(2H, s), 6.08(1H, d, J=9.0Hz), 6.34(2H, t,J=2.4Hz), 7.16(2H, t, J=2.4Hz), 7.28(1H, d, J=3.9Hz), 7.57(1H, d,J=3.9Hz); IR (CHCl₃) 3512, 3446, 1709, 1657, 1504, 1456, 1385, 1192,1167, 1057, 1034cm⁻¹; [α]_(D) ^(25.0)+26.2±0.7°(c=1.008, MeOH)Anal.(C₂₃H₃₀N₂O₅S₂.0.6H₂O.0.3AcOEt) Calcd.(%): C, 56.33; H, 6.65; N,5.45; S, 12.40 Found(%): C, 56.31; H, 6.35; N, 5.64; S, 12.08 II-5A-31a¹H-NMR(CDCl₃) δ 0.90(1H, d, J=10.2Hz), 1.08(3H, s), 1.20(3H, s),1.30–2.38(14H, m), 4.13(2H, s), 4.18(1H, m), 5.93(1H, d, J=10.2Hz),6.77(1H, d, J=3.6Hz), 7.20–7.38(6H, m); IR(CHCl₃) 3512, 3450, 3431,1709, 1643, 1543, 1506, 1456cm⁻¹; [α]_(D) ^(24.0)+20.4±0.6° (c=1.011,MeOH) Anal.(C₂₆H₃₃NO₃S.0.6H₂O) Calcd.(%): C, 71.04; H, 7.57; N, 3.19; S,7.29 Found(%): C, 69.33; H, 7.65; N, 3.31; S, 7.11 II-5A-47a¹H-NMR(CDCl₃) δ 0.91(1H, d, J=10.8Hz), 1.08(3H, s), 1.21(3H, s),1.30–2.38(14H, m), 4.19(1H, m), 6.08(1H, d, J=9.3Hz), 7.11(1H, dd,J=5.1, 3.9Hz), 7.32(1H, d, J=3.9Hz), 7.64(1H, d, J=3.9Hz), 7.69(1H, dd,J= 5.1, 1.2Hz), 7.75(1H, dd, J=3.6, 1.2Hz); IR(CHCl₃) 3516, 3446, 2679,1709, 1655, 1529, 1504, 1402, 1336, 1153, 1095, 1074, 1024cm⁻¹; [α]_(D)^(24.0)+23.5±0.6° (c=1.004, MeOH) Anal.(C₂₃H₂₉NO₅S₃.0.5H₂O) Calcd.(%):C, 54.74; H, 5.99; N, 2.78; S, 19.06 Found(%): C, 54.90; H, 5.76; N,2.85; S, 18.81 II-5A-55a ¹H-NMR(CDCl₃) δ 0.91(1H, d, J=10.2Hz), 1.09 and1.22(3H, s), 1.22–2.30(12H, m), 2.33(2H, t, J=7.5Hz), 2.39(3H, s),4.19(1H, m), 5.99(1H, m), 6.09(1H, d, J= 8.7Hz), 6.20(1H, t, J=3.3Hz),7.19(1H, dd, J=1.8, 6.3Hz), 7.29(1H, d, J=3.9Hz), 7.55(1H, d, J=3.9Hz);IR (CHCl₃) 3446, 1709, 1657, 1529, 1504, 1375, 1205, 1182, 1161,1053cm⁻¹; [α]_(D) ²⁴+25.3±0.7°(c=1.002, MeOH) Anal.(C₂₄H₃₂N₂O₅S₂)Calcd.(%): C, 58.51; H, 6.55; N, 5.69; S, 13.02 Found(%): C, 58.21; H,6.53; N, 5.69; S, 12.93

TABLE 45 Compd. No.. Physical property II-5A-55c ¹H-NMR(CDCl₃) δ0.89(1H, d, J=10.5Hz), 1.08(3H, s), 1.22(3H, s), 1.36–2.36(14H, m),2.39(3H, s), 4.16(1H, m), 5.24(1H, brs), 5.50(1H, brs), 5.99(1H, m),6.20(1H, t, J=3.3Hz), 6.20(1H, brs), 7.19(1H, m), 7.32(1H, d, J= 4.2Hz),7.56(1H, d, J=4.2Hz); IR(CHCl₃) 3529, 3446, 3411, 3348, 1678, 1591,1529, 1504, 1375, 1182, 1161, 1144, 1053cm⁻¹; [α]_(D)^(26.0)+23.0±0.6°(c=1.016, MeOH) Anal.(C₂₄H₃₃N₃O₄S₂.0.4H₂O) Calcd.(%):C, 57.78; H, 6.83; N, 8.42; S, 12.86 Found(%): C, 57.79; H, 6.81; N,8.37; S, 12.68 II-5A-55g ¹H-NMR(CDCl₃) δ 0.89(1H, d, J=10.5Hz), 1.12(3H,s), 1.25(3H, s), 1.33–2.35(12H, m), 2.39(3H, s), 2.95–3.11 (2H, m),4.19(1H, m), 6.00(1H, m), 6.21(1H, t, J=3.3Hz), 6.45(1H, d, J=8.7Hz),7.18(1H, dd, J=3.3, 1.5Hz), 7.38(1H, d, J=3.9Hz), 7.54(1H, d, J=3.9Hz);IR (CHCl₃) 3149, 2624, 1641, 1533, 1508, 1375, 1205, 1182, 1160cm⁻¹;[α]_(D) ^(25.0)+17.9±0.6°(c=1.018, MeOH) Anal. (C₂₄H₃₂N₆O₃S₂.0.4CHCl₃)Calcd.(%): C, 51.62; H, 5.79; N, 14.89; S, 11.36 Found(%): C, 51.53; H,5.99; N, 14.82; S, 11.09 II-5A-59a ¹H-NMR(CDCl₃) δ 0.90(1H, d,J=10.2Hz), 1.07(3H, s), 1.21(3H, s), 1.28–2.36(14H, m), 4.17(1H, m),5.91(1H, d, J=8.4Hz), 7.00(1H, dd, J=5.4, 3.6Hz), 7.05(1H, d, J=3.9Hz),7.25(1H, d, J=3.9Hz), 7.28(1H, dd, J= 3.6, 1.2Hz), 7.42(1H, dd, J=5.4,1.2Hz); IR(CHCl₃) 3516, 3450, 3431, 2671, 1709, 1645, 1529, 1500, 1471,1421cm⁻¹; [α]_(D) ^(25.0)+23.3±0.6°(c=1.013, MeOH) Anal.(C₂₃H₂₉NO₃S₃.0.2H₂O) Calcd.(%): C, 59.12; H, 6.34; N, 3.00; S, 20.58Found(%): C, 59.12; H, 6.30; N, 3.07; S, 20.84 II-5A-88a ¹H-NMR(CDCl₃) δ0.91(1H, d, J=10.2Hz), 1.09(3H, s), 1.21(3H, s), 1.18–2.33(14H, m),4.15(2H, s), 4.19(1H, m), 5.94(1H, d, J=9.6Hz), 6.79(1H, d, J=3.6Hz),6.96(1H, dd, J=5.1, 1.2Hz), 7.05(1H, dd, J=1.8, 1.2Hz), 7.28(1H, dd,J=5.1, 1.8Hz), 7.30(1H, d, J=3.6Hz); IR(CHCl₃) 3516, 3450, 3431, 1709,1641, 1545, 1506, 1471cm⁻¹; [α]_(D) ^(24.0)+19.6±0.6°(c=1.009, MeOH)Anal.(C₂₄H₃₁NO₃S₂.0.3H₂O) Calcd.(%): C, 63.91; H, 7.06; N, 3.11; S,14.22 Found(%): C, 63.89; H, 6.89; N, 3.31; S, 14.28 II-5A-104a¹H-NMR(CDCl₃) δ 0.92(1H, d, J=10.2Hz), 1.10(3H, s), 1.22(3H, s),1.28–2.38(14H, m), 4.10(2H, s), 4.20(1H, m), 5.97(1H, d, J=9.6Hz),6.70(1H, d, J=3.6Hz), 6.95(1H, m), 7.04(1H, dd, J=3.3, 1.2Hz), 7.24(1H,d, J= 3.6Hz), 7.37(1H, dd, J=5.1, 1.2Hz); IR(CHCl₃) 3516, 3450, 2669,1709, 1643, 1543, 1508, 1471cm⁻¹; [α]_(D) ^(25.0)+ 20.8±0.6°(c=1.015,MeOH) Anal.(C₂₄H₃₁NO₃S_(3.) 0.3H₂O) Calcd.(%): C, 59.67; H, 6.59; N,2.90; S, 19.91 Found(%): C, 59.65; H, 6.49; N, 3.13; S, 20.18

TABLE 46 Compd. No.. Physical property II-5A-143a ¹H-NMR(CDCl₃) δ0.95(1H, d, J=9.9Hz), 1.04(3H, s), 1.23(3H, s), 1.32–2.40(14H, m),4.24(2H, s), 4.32(1H, m), 6.11(1H, d, J=9.0Hz), 7.16–7.32(6H, m),7.42(1H, dd, J=8.1, 7.2Hz), 7.76(1H, s), 8.18(1H, d, J=8.1Hz); IR(CHCl₃)3516, 3442, 1709, 1651, 1513, 1495, 1471cm⁻¹; [α]_(D)^(24.0)+31.6±0.7°(c=1.000, MeOH) Anal. (C₃₀H₃₅NO₃S.0.3H₂O) Calcd.(%): C,72.78; H, 7.25; N, 2.83; S, 6.48 Found(%): C, 72.79; H, 7.27; N, 2.87;S, 6.44 II-5A-197a ¹H-NMR(CDCl₃) δ 0.90(1H, d, J=9.9Hz), 1.08(3H, s),1.20(3H, s), 1.30–2.36(14H, m), 3.22(2H, t, J=9.0Hz), 4.07(2H, s),4.18(1H, m), 4.57(2H, t, J=9.0Hz), 5.92 (1H, d, J=8.4Hz), 6.78(1H, t,J=7.5Hz), 6.80(1H, d, J= 3.9Hz), 6.95(1H, d, J=7.5Hz), 7.09(1H, d,J=7.5Hz), 7.28(1H, d, J=3.9Hz); IR(CHCl₃) 3516, 3450, 3431, 1709, 1641,1543, 1506, 1458cm⁻¹; [α]_(D) ^(25.0)+ 41.1±0.8°(c=1.002, MeOH)Anal.(C₂₈H₃₅NO₄S.0.3H₂O) Calcd.(%): C, 69.05; H, 7.37; N, 2.88; S, 6.58Found(%): C, 69.05; H, 7.20; N, 3.06; S, 6.51 II-5B-55a ¹H-NMR(CDCl₃) δ0.93(1H, d, J=10.5Hz), 1.08 and 1.23(3H, s), 1.55(1H, m), 1.91–2.42(7H,m), 2.39(3H, s), 3.18(2H, d, J=6.6Hz), 4.20(1H, m), 5.56–5.73(2H, m),5.99(1H, m), 6.18–6.23(2H, m), 7.19(1H, dd, J=1.5, 3.3Hz), 7.30(1H, d,J=3.9Hz), 7.54(1H, d, J=3.9Hz); IR(CHCl₃) 3446, 1711, 1657, 1529, 1504,1375, 1182, 1161, 1144, 1053cm⁻¹; [α]_(D) ²⁵+38.8±0.8°(c=1.001, MeOH)Anal.(C₂₄H₃₉N₂O₅S₂.0.3H₂O) Calcd.(%): C, 58.11; H, 6.22; N, 5.65; S,12.93 Found(%): C, 58.13; H, 6.09; N, 5.68; S, 12.73. II-5C-1a¹H-NMR(CDCl₃) δ 0.95(1H, d, J=10.5Hz), 1.08(3H, s), 1.23(3H, s),1.42–2.33(10H, m), 4.22(1H, m), 5.78(1H, d, J= 15.9Hz), 6.07(1H, d,J=8.1Hz), 6.33(2H, t, J= 2.4Hz), 7.03(1H, dt, J=15.9, 6.9Hz), 7.16(2H,t, J= 2.4Hz), 7.28(2H, d, J=4.2Hz), 7.57(1H, d, J=4.2Hz); IR(CHCl₃)3523, 3446, 1697, 1655, 1529, 1504, 1456, 1385, 1192, 1167, 1057,1034cm⁻¹; [α]_(D) ^(25.0)+29.7±0.7° (c=1.005, MeOH)Anal.(C₂₃H₂₈N₂O₅S₂.0.2H₂O) Calcd.(%): C, 57.52; H, 5.96; N, 5.83; S,13.35 Found(%): C, 57.51; H, 5.89; N, 5.88; S, 13.31 II-5C-55a¹H-NMR(CDCl₃) δ 0.92(1H, d, J=10.5Hz), 1.09 and 1.23(3H, s),1.48–2.40(10H, m), 2.39(3H, s), 4.24(1H, m), 5.79(1H, d, J=15.6Hz),5.99(1H, m), 6.09(1H, d, J= 8.7Hz), 6.20(1H, t, J=3.6Hz), 7.03(1H, dt,J=6.9, 15.6Hz), 7.19(1H, dd, J=1.8, 3.3Hz), 7.29(1H, d, J= 4.2Hz),7.55(1H, d, J=4.2Hz).; IR(CHCl₃) 3446, 1697, 1655, 1529, 1504, 1375,1182, 1161, 1144, 1053cm⁻¹; [α]_(D) ^(26.5)+27.9±0.7°(c=1.005, MeOH)Anal. (C₂₄H₃₉N₂O₅S₂.0.3H₂O) Calcd.(%): C, 58.11; H, 6.22; N, 5.65; S,12.93 Found(%): C, 58.12; H, 6.22; N, 5.62; S, 12.91.

TABLE 47 Compd. No.. Physical property II-5E-1a mp 154–155° C.;¹H-NMR(CDCl₃) δ 0.90(1H, d, J=10.2Hz), 1.10 and 1.23(3H, s), 1.51(1H,ddd, J=2.1, 5.1, 12.9Hz), 1.72–2.40(7H, m), 3.58–3.64(2H, m), 3.98 and4.07(each 1H, Abq, J=16.8Hz), 4.23(1H, m), 6.27(1H, d, J=8.7Hz),6.32–6.35(2H, m), 7.15–7.17(2H, m), 7.31(1H, d, J=3.9Hz), 7.55(1H, d,J=3.9Hz); IR(CHCl₃) 3444, 1730, 1655, 1529, 1504, 1456, 1385, 1192,1167, 1057, 1034cm⁻¹; [α]_(D) ²⁴ −2.2±0.4°(c=1.009, MeOH)Anal.(C₂₂H₂₈N₂O₆S₂) Calcd.(%): C, 54.98 H, 5.87; N, 5.83; S, 13.34Found(%): C, 54.97; H, 5.92; N, 5.89; S, 13.12 II-5E-55a ¹H-NMR(CDCl₃) δ0.90(1H, d, J=9.9Hz), 1.10 and 1.23 (3H, s), 1.51(1H, ddd, J=2.7, 4.8,12.6Hz), 1.74–2.40(7H, m), 2.39(3H, s), 3.58–3.64(2H, m), 3.98 and4.07(each 1H, Abq, J=17.1Hz), 4.23(1H, m), 5.99(1H, m), 6.20(1H, t, J=3.6Hz), 6.29(1H, d, J=8.1Hz), 7.19(1H, dd, J=1.5, 3.3Hz), 7.33(1H, d,J=3.9Hz), 7.53(1H, d, J=3.9Hz); IR (CHCl₃) 3444, 1729, 1655, 1529, 1504,1375, 1182, 1161, 1142, 1053cm⁻¹; [α]_(D) ²⁴ −2.8±0.4°(c=1.013, MeOH)Anal. (C₂₃H₃₀N₂O₆S₂.1.2H₂O) Calcd.(%): C, 53.51; H, 6.33; N, 5.43; S,12.42 Found(%): C, 53.53; H, 5.93; N, 5.45; S, 12.55 II-5F-31a¹H-NMR(CDCl₃) δ 0.90(1H, d, J=10.2Hz), 1.09 and 1.22 (3H, s), 1.47(1H,ddd, J=2.4, 4.8, 12.9Hz), 1.74(1H, m), 1.91–2.38(6H, m), 2.61–2.80(2H,m), 3.49(2H, s), 4.13(2H, s), 4.21(1H, m), 6.07(1H, d, J=8.4Hz),6.77(1H, dt, J=0.9, 3.6Hz), 7.22–7.35(6H, m); IR(CHCl₃) 2924, 1711,1641, 1543, 1508, 1471, 1454, 1286, 1257, 1227, 1223cm⁻¹; [α]_(D) ²⁶⁺30.7±1.4°(c=0.512%, MeOH); Anal.(C₂₅H₃₁NO₃S₂.0.3H₂O) Calcd.(%) C, 64.85;H, 6.88; N, 3.02; S, 13.85 Found(%) C, 64.73; H, 6.81; N, 3.13; S, 13.81II-5F-55a ¹H-NMR(CDCl₃) δ 0.90(1H, d, 10.2Hz), 1.10 and 1.23(3H, s),1.49(1H, ddd, J=2.7, 5.7, 13.5Hz), 1.64–2.38(7H, m), 2.39(3H, s),2.60–2.80(2H, m), 3.21(2H, ABq, J=15.0Hz), 4.19(1H, m), 5.98(1H, m),6.20(1H, t, J=3.0Hz), 6.25(1H, d, J=8.4Hz), 7.18(1H, m), 7.33(1H, d,J=4.2Hz), 7.53 (1H, d, J=4.2Hz); IR(CHCl₃) 2925, 1710, 1657, 1529, 1504,1375, 1227, 1213, 1207, 1182, 1161cm⁻¹; [α]_(D) ²⁶+29.6±1.4° (c=0.503%,MeOH); Anal.(C₂₃H₃₀N₂O₅S₃.0.4H₂O) Calcd.(%) C, 53.34; H, 5.99; N, 5.41;S, 18.57 Found(%) C, 53.41; H, 6.01; N, 5.47; S, 18.65 II-5F-88a¹H-NMR(CDCl₃) δ 0.91(1H, d, 10.2Hz), 1.10 and 1.22(3H, s), 1.48(1H, m),1.67–2.38(7H, m), 2.60–2.80(2H, m), 3.21 (2H, br s), 4.18(2H, d,J=0.9Hz), 4.22(1H, m), 6.08(1H, d, J=8.4Hz), 6.79(1H, dt, J=0.9, 3.6Hz),6.96(1H, dd, J= 1.5, 5.1Hz), 7.05(1H, m), 7.27–7.33(2H, m); IR(CHCl₃)2923, 1710, 1643, 1543, 1508, 1471, 1286, 1221, 1205cm⁻¹; [α]_(D)²⁶+30.3±1.4°(c=0.508%, MeOH); Anal. (C₂₃H₂₉NO₃S₃.0.2H₂O) Calcd.(%) C,59.12; H, 6.34; N, 3.00; S, 20.59 Found(%) C, 59.10; H, 6.31; N, 3.09;S, 20.47

TABLE 48 Compd. No.. Physical property II-6A-55a ¹H-NMR(CDCl₃) δ0.88(1H, d, J=10.2Hz), 1.08 and 1.21(3H, s), 1.22–2.36(16H, m), 2.38(3H,s), 4.16(1H, m), 5.98(1H, m), 6.19(1H, t, J=3.3Hz), 6.30(1H, d, J=8.7Hz), 7.17(1H, dd, J=1.8, 3.3Hz), 7.33(1H, d, J= 4.2Hz), 7.52(1H, d,J=4.2Hz); IR(CHCl₃) 3446, 1709, 1657, 1529, 1504, 1375, 1182, 1161,1144, 1053cm⁻¹; [α]_(D) ²⁵+22.7±0.6°(c=1.002, MeOH) Anal.(C₂₅H₃₄N₂O₅S₂.0.3H₂O) Calcd.(%): C, 58.64; H, 6.81; N, 5.47; S, 12.52Found(%): C, 58.73; H, 6.68; N, 5.45; S, 11.93. II-6B-55a ¹H-NMR(CDCl₃)δ 0.94(1H, d, J=10.5Hz), 1.08 and 1.22(3H, s), 1.55(1H, ddd, J=2.4, 5.7,13.2Hz), 1.84–2.50 (11H, m), 2.39(3H, s), 4.20(1H, m), 5.37–5.52(2H, m),5.99(1H, m), 6.17–6.21(2H, m), 7.18(1H, dd, J=1.8, 6.3Hz), 7.31(1H, d,J=4.2Hz), 7.54(1H, d, J=4.2Hz); IR(CHCl₃) 3446, 1711, 1657, 1529, 1504,1392, 1375, 1182, 1161, 1144, 1053cm⁻¹; [α]_(D) ²⁵+44.6±0.8°(c=1.004,MeOH) Anal.(C₂₅H₃₂N₂O₅S₂) Calcd.(%): C, 59.50; H, 6.39; N, 5.55; S,12.71 Found(%): C, 59.16; H, 6.27; N; 5.54; S, 12.44 II-7A-31a¹H-NMR(CDCl₃) δ 0.91(1H, d, J=9.9Hz), 1.08(3H, s), 1.20(3H, s),1.22–2.34(18H, m), 4.13(2H, s), 4.19(1H, m), 5.92(1H, d, J= 9.0Hz),6.77(1H, d, J=3.6Hz), 7.22–7.35(6H, m); IR(CHCl₃) 3516, 3450, 3431,1709, 1641, 1545, 1506, 1469, 1456cm⁻¹; [α]_(D) ^(24.0)+20.4±0.6°(c=1.000, MeOH) Anal.(C₂₈H₃₇NO₃S.0.2H₂O) Calcd.(%): C, 71.36; H, 8.00;N, 2.97; S, 6.80 Found(%): C, 71.44; H, 7.99; N, 3.02; S, 6.69 II-7A-47a¹H-NMR(CDCl₃) δ 0.91(1H, d, J=10.5Hz), 1.09(3H, s), 1.21(3H, s),1.22–2.33(18H, m), 4.19(1H, m), 6.06(1H, d, J= 9.0Hz), 7.11(1H, dd,J=5.1, 3.9Hz), 7.33(1H, d, J=3.9Hz), 7.65(1H, d, J=3.9Hz), 7.70(1H, dd,J= 5.1, 1.5Hz), 7.76(1H, dd, J=3.6, 1.5Hz); IR(CHCl₃) 3516, 3446, 2679,1709, 1657, 1529, 1504, 1402, 1336, 1153, 1095, 1022cm⁻¹; [α]_(D)^(24.0) 30 25.3±0.7°(c=1.004, MeOH) Anal.(C₂₅H₃₃NO₅S₃.0.3H₂O) Calcd.(%):C, 56.75; H, 6.40; N, 2.65; S, 18.07 Found(%): C, 56.88; H, 6.43; N,2.68; S, 17.79 II-7A-55a ¹H-NMR(CDCl₃) δ 0.90(1H, d, J=10.2Hz), 1.08 and1.22(3H, s), 1.22–2.32(18H, m), 2.39(3H, s), 4.18(1H, m), 4.65(1H, brs), 5.99(1H, m), 6.12(1H, d, J=9.0Hz), 6.20(1H, t, J=3.6Hz), 7.03(1H,dt, J=6.9, 15.6Hz), 7.19(1H, dd, J=1.8, 3.3Hz), 7.30(1H, d, J=4.2Hz),7.54(1H, d, J=3.9Hz); IR(CHCl₃) 3446, 1708, 1657, 1529, 1504, 1375,1182, 1161, 1144, 1053cm⁻¹; [α]_(D) ²⁵+25.1±0.6°(c=1.009, MeOH) Anal.(C₂₆H₃₆N₂O₅S₂.0.2H₂O) Calcd.(%): C, 59.56; H, 7.00; N, 5.34; S, 12.23Found(%): C, 59.59; H, 7.01; N, 5.33; S, 11.85.

TABLE 49 Compd. No.. Physical property II-7A-55e ¹H-NMR(CDCl₃) δ0.93(1H, d, J=10.2Hz), 1.10(3H, s), 1.23(3H, s), 1.32–2.34(16H, m),2.29(2H, d, J=7.5Hz), 2.39(3H, s), 3.28(3H, s), 4.21(1H, m), 6.00(1H,m), 6.17(1H, d, J=9.3Hz), 6.21(1H, m), 7.19(1H, m), 7.36 (1H, d,J=3.9Hz), 7.56(1H, d, J=3.9Hz), 8.76(1H, br); IR(CHCl₃) 3386, 2927,2862, 1718, 1651, 1531, 1506, 1398, 1375, 1344, 1159, 1053, 1020cm⁻¹;[α]_(D) ²⁴+20.8±0.6°(c=1.00, MeOH) Anal. (C₂₇H₃₉N₃O₆S₃.0.5MeOH)Calcd.(%): C, 53.81; H, 6.73; N, 6.85; S, 15.67 Found(%): C, 53.91; H,6.64; N, 7.13; S, 15.29 II-7A-55g ¹H-NMR(CDCl₃) δ 0.94(1H, d, J=10.5Hz),1.13(3H, s), 1.25(3H, s), 1.26–2.40(16H, m), 2.38(3H, s), 2.93–3.00 (2H,m), 4.28(1H, m), 6.00(1H, m), 6.21(1H, t, J=3.3Hz), 6.43(1H, d,J=8.7Hz), 7.17(1H, dd, J=3.3, 1.5Hz), 7.42(1H, d, J=3.9Hz), 7.56(1H, d,J=3.9Hz); IR (CHCl₃) 3426, 2626, 1639, 1533, 1508, 1375, 1222, 1216,1205, 1184, 1160cm⁻¹; [α]_(D) ^(24.0)+22.7±0.6°(c=1.002, MeOH)Anal.(C₂₆H₃₆N₆O₃S₂.0.6H₂O) Calcd.(%): C, 56.21; H, 6.75; N, 15.03; S,11.43 Found(%): C, 56.32; H, 6.52; N, 14.80; S, 11.13 II-7A-59a¹H-NMR(CDCl₃) δ 0.90(1H, d, J=10.2Hz), 1.07(3H, s), 1.20(3H, s),1.24–2.33(18H, m), 4.17(1H, m), 5.91(1H, d, J= 9.0Hz), 7.00(1H, dd,J=5.4, 3.6Hz), 7.05(1H, d, J=3.6Hz), 7.26(1H, d, J=3.6Hz), 7.28(1H, dd,J= 3.6, 1.2Hz), 7.42(1H, dd, J=5.4, 1.2Hz); IR(CHCl₃) 3516, 3450, 3431,2673, 1709, 1645, 1529, 1500, 1471, 1421cm⁻¹; [α]_(D)^(25.0)+20.1±0.6°(c=1.010, MeOH) Anal. (C₂₅H₃₃NO₃S₃) Calcd.(%): C,61.06; H, 6.76; N, 2.85; S, 19.56 Found(%): C, 60.86; H, 6.87; N, 2.93;S, 19.29 II-7A-88a ¹H-NMR(CDCl₃) δ 0.91(1H, d, J=10.2Hz), 1.09(3H, s),1.21(3H, s), 1.24–2.33(18H, m), 4.15(2H, s), 4.19(1H, m), 5.94(1H, d, J=9.0Hz), 6.79(1H, d, J=3.6Hz), 6.96 (1H, dd, J=5.1, 1.2Hz), 7.05(1H, m),7.27(1H, dd, J= 4.8, 1.2Hz), 7.30(1H, d, J=3.6Hz); IR(CHCl₃) 3518, 3450,3431, 1709, 1641, 1545, 1506, 1469cm⁻¹; [α]_(D)^(24.0)+19.2±0.6°(c=1.012, MeOH) Anal. (C₂₆H₃₅NO₃S₂.0.1H₂O) Calcd.(%):C, 65.67; H, 7.46; N, 2.95; S, 13.09 Found(%): C, 65.81; H, 7.43; N,2.94; S, 12.99 II-7A- ¹H-NMR(CDCl₃) δ 0.92(1H, d, J=10.5Hz), 104a1.10(3H, s), 1.22(3H, s), 1.25–2.34(18H, m), 4.10(2H, s), 4.20(1H, m),5.95(1H, d, J=8.7Hz), 6.70(1H, d, J=3.3Hz), 6.95(1H, dd, J=5.1, 3.9Hz),7.04(1H, dd, J=3.9, 1.2Hz), 7.25(1H, d, J=3.3Hz), 7.36(1H, dd, J=5.1,1.2Hz); IR(CHCl₃) 3516, 3450, 3431, 1709, 1643, 1543, 1506, 1471cm⁻¹;[α]_(D) ^(25.0)+19.8±0.6°(c=1.009, MeOH) Anal.(C₂₆H₃₅NO₃S₃.0.1H₂O)Calcd.(%): C, 61.53, H, 6.99, N, 2.76; S, 18.95 Found(%): C, 61.42; H,6.85; N, 2.86; S, 18.89

TABLE 50 Compd. No.. Physical property II-7A-143a ¹H-NMR(CDCl₃) δ0.96(1H, d, J=10.2Hz), 1.10(3H, s), 1.23(3H, s), 1.26–2.38(18H, m),4.24(2H, s), 4.32(1H, m), 6.11(1H, d, J= 8.7Hz), 7.19–7.28(6H, m),7.42(1H, dd, J=8.1, 7.2Hz), 7.76(1H, s), 8.19(1H, d, J=8.1Hz); IR(CHCl₃)3516, 3442, 1709, 1651, 1514, 1495, 1469cm⁻¹; [α]_(D)^(24.0)+34.1±0.7°(c=1.004, MeOH) Anal. (C₃₂H₃₉NO₃S.0.2H₂O) Calcd.(%): C,73.73; H, 7.62; N, 2.69; S, 6.15 Found(%): C, 73.72; H, 7.68; N, 2.65;S, 5.88 II-7A-197a ¹H-NMR(CDCl₃) δ 0.91(1H, d, J=9.9Hz), 1.08(3H, s),1.20(3H, s), 1.24–2.33(18H, m), 3.22(2H, t, J=8.7Hz), 4.05(2H, s),4.19(1H, m), 4.57(2H, t, J=8.7Hz), 5.92 (1H, d, J=9.3Hz), 6.79(1H, t,J=7.2Hz), 6.80(1H, d, J= 3.9Hz), 6.96(1H, d, J=7.2Hz), 7.09(1H, d,J=7.2Hz), 7.28(1H, d, J=3.9Hz); IR(CHCl₃) 3516, 3450, 3431, 2671, 1709,1639, 1543, 1506, 1458cm⁻¹; [α]_(D) ^(25.0)+ 17.4±0.6°(c=1.001, MeOH)Anal.(C₃₀H₃₉NO₄S.0.3H₂O) Calcd.(%): C, 69.95; H, 7.75; N, 2.72; S, 6.22Found(%): C, 69.86; H, 7.65; N, 2.80; S, 6.08 II-7A-315a ¹H-NMR(CDCl₃) δ0.96(1H, d, J=9.9Hz), 1.11(3H, s), 1.24(3H, s), 1.33–2.36(16H, m),2.3(2H, t, J=7.2Hz), 4.26(2H, s), 4.33(1H, m), 6.12(1H, d, J=9.3Hz),7.00–7.23(5H, m), 7.42(1H, m), 7.78(1H, s), 8.20(1H, d, J=7.5Hz);IR(CHCl₃) 3516, 3442, 2925, 2858, 1709, 1651, 1585, 1570, 1514, 1492,1469, 1396cm⁻¹; [α]_(D) ^(25.5)+33.4±0.7°(c=1.00, MeOH) Anal.(C₃₂H₃₈FNO₃S.0.5MeOH) Calcd.(%): C, 70.75; H, 7.31; N, 2.54; F, 3.44; S,5.81 Found(%): C, 70.85; H, 7.34; N, 2.80; F, 3.06; S, 5.66 II-7A-316a¹H-NMR(CDCl₃) δ 0.96(1H, d, J=10.2Hz), 1.11(3H, s), 1.24(3H, s),1.32–2.36(16H, m), 2.30(2H, t, J=7.2Hz), 3.82(3H, s), 4.23(2H, s),4.33(1H, m), 6.12(1H, d, J= 9.0Hz), 6.82–6.91(2H, m), 7.05–7.22(3H, m),7.39(1H, m), 7.78(1H, s), 8.14(1H, d, J=8.1Hz); IR(CHCl₃) 3516, 3442,2925, 2858, 1709, 1651, 1601, 1514, 1493, 1468, 1439, 1394, 1246cm⁻¹;[α]_(D) ^(26.0)+31.4±0.7°(c=1.04, MeOH) Anal.(C₃₃H₄₁NO₄S.0.1H₂O)Calcd.(%): C, 72.12; H, 7.56; N, 2.55; S, 5.23 Found(%): C, 71.93; H,7.73; N, 2.77; S, 5.60 II-7B-55a ¹H-NMR(CDCl₃) δ 0.91(1H, d, J=10.2Hz),1.08(3H, s), 1.15(3H, d, J=7.2Hz), 1.22(3H, s), 1.29–2.45(17H, m),2.39(3H, s), 4.19(1H, m), 5.98(1H, d, J=2.4Hz), 6.06 (1H, d, J=9.0Hz),6.20(1H, dd, J=3.3 and 3.6Hz), 7.19(1H, dd, J=2.4 and 3.3Hz), 7.29(1H,d, 3.9Hz), 7.55(1H, d, J=3.9Hz); IR(CHCl₃) 3448, 2927, 2860, 1739, 1705,1657, 1529, 1504, 1469, 1375, 1281, 1161, 1144, 1070, 1053, 1022cm⁻¹;[α]_(D) ²⁴+21.4±0.6°(c=1.02, MeOH) Anal.(C₂₇H₃₈N₂O₅S₂.0.3H₂O) Calcd.(%):C, 60.04; H, 7.20; N, 5.19; S, 11.87 Found(%): C, 60.26; H, 7.22; N,5.28; S, 11.50

TABLE 51 Compd. No.. Physical property II-7E-55c ¹H-NMR(CDCl₃) δ0.93(1H, d, J=10.5Hz), 1.08(3H, s), 1.21(3H, s), 1.50–2.40(14H, m),2.39(3H, s), 4.14(1H, m), 5.24(1H, brs), 5.33–5.50(2H, m), 5.99(1H, m),5.99(1H, brs), 6.20(1H, t, J=3.3Hz), 6.48(1H, d, J=7.2Hz), 7.19 (1H, m),7.39(1H, d, J=4.2Hz), 7.55(1H, t, J=4.2Hz); IR(CHCl₃) 3527, 3485, 3448,3411, 3348, 1676, 1591, 1529, 1504, 1375, 1182, 1161, 1144, 1053cm⁻¹;[α]_(D) ^(26.0)+55.5±1.0° (c=1.010, MeOH) Anal.(C₂₆H₃₅N₃O₄S₂.0.3H₂O)Calcd.(%): C, 59.70; H, 6.86; N, 8.03; S, 12.26 Found(%): C, 59.79; H,6.75; N, 8.05; S, 12.14 II-7E-55e mp 70–72° C.; ¹H-NMR(CDCl₃) δ 0.96(1H,d, J=10.8Hz), 1.09(3H, s), 1.22(3H, s), 1.60–2.37(14H, m), 2.41(3H, s),3.25(3H, s), 4.10(1H, m), 5.28–5.47(2H, m), 6.00(1H, m), 6.06(1H, d,J=8.7Hz), 6.22(1H, dd, J=3.3 and 3.6Hz), 7.19(1H, dd, J=1.8 and 3.3Hz),7.41(1H, d, J=3.9Hz), 7.57(1H, d, J=3.9Hz); IR(CHCl₃ ) 3427, 3386, 2927,1714, 1647, 1531, 1506, 1454, 1375, 1342, 1161, 1120, 1053, 1020cm⁻¹;[α]_(D) ²⁴+50.0±0.9°(c=1.00, MeOH) Anal. (C₂₇H₃₇N₃O₆S₃.0.4H₂O)Calcd.(%): C, 53.78; H, 6.32; N, 6.97; S, 15.95 Found(%): C, 53.89; H,6.28; N, 7.05; S, 15.57 II-7E-55g ¹H-NMR(CDCl₃) δ 0.76(1H, d, J=10.8Hz),1.10(3H, s), 1.24(3H, s), 1.44–2.31(12H, m), 2.40(3H, s), 2.92–3.08 (2H,m), 3.98(1H, m), 5.37–5.39(2H, m), 6.01(1H, m), 6.22 (1H, t, J=3.3Hz),6.30(1H, d, J=8.4Hz), 7.19(1H, dd, J= 3.3, 1.8Hz), 7.41(1H, d, J=3.9Hz),7.58(1H, d, J=3.9Hz); IR(CHCl₃) 3151, 1639, 1533, 1508, 1375, 1184,1160cm⁻¹; [α]_(D) ^(25.0)+40.9±0.8°(c=1.010, MeOH) Anal. (C₂₆H₃₄N₆O₃S₂.1.3H₂O) Calcd.(%): C, 55.16; H, 6.52; N, 14.44; S, 10.43 Found(%): C,55.44; H, 6.42; N, 14.17; S, 10.66 II-7F-55a ¹H-NMR(CDCl₃) δ 0.94(1H, d,J=9.9Hz), 1.08(3H, s), 1.16 or 1.18(3H, d, J=4.2Hz), 1.22(3H, s),1.47–2.52 (13H, m), 2.39(3H, s), 4.20(1H, m), 5.38–5.41(2H, m), 5.99(1H,m), 6.14–6.21(2H, m), 7.19(1H, m), 7.31(1H, m), 7.54(1H, m); IR(CHCl₃)3446, 2925, 2870, 1738, 1705, 1657, 1529, 1504, 1469, 1375, 1182, 1161,1144, 1070, 1053, 1022cm⁻¹; [α]_(D) ²⁴+49.8±0.9°(c=1.02, MeOH) Anal.(C₂₇H₃₆N₂O₅S₂.0.4H₂O) Calcd.(%): C, 60.06; H, 6.87; N, 5.19; S, 11.88Found(%): C, 60.03; H, 6.71; N, 5.31; S, 11.76 II-7I-1a mp 111–115° C.;¹H-NMR(CDCl₃) δ 0.91(1H, d, J=10.5Hz), 1.09 and 1.22(3H, s),1.22–2.40(12H, m), 4.19(1H, m), 5.79(1H, br d, J=15.6Hz), 6.06(1H, d,J=9.3Hz), 6.32–6.35(2H, m), 7.03(1H, dt, J=7.8, 15.6Hz), 7.15–7.17 (2H,m), 7.27(1H, d, J=3.9Hz), 7.57(1H, d, J=3.9Hz); IR(CHCl₃) 3446, 1695,1654, 1529, 1504, 1456, 1385, 1192, 1167, 1057, 1034cm⁻¹; [α]_(D)²⁵+20.5±0.6°(c=1.007, MeOH) Anal.(C₂₅H₃₂N₂O₅S₂) Calcd.(%): C, 59.50; H,6.39; N, 5.55; S, 12.71 Found(%): C, 59.19; H, 6.39; N, 5.48; S, 12.39

TABLE 52 Compd. No.. Physical property II-7I-47a ¹H-NMR(CDCl₃) δ0.91(1H, d, J=10.8Hz), 1.09 and 1.22(3H, s), 1.22–2.40(12H, m), 4.20(1H,m), 5.79(1H, br d, J=15.6Hz), 5.99(1H, m), 6.08(1H, d, J=9.0Hz),7.03(1H, dt, J=7.2, 15.6Hz), 7.11(1H, dd, J=3.9, 5.1Hz), 7.33(1H, d,J=3.9Hz), 7.65(1H, d, J=3.9Hz) 7.70 (1H, dd, J=1.2, 6.0Hz), 7.76(1H, dd,J=1.2, 3.9Hz); IR(CHCl₃) 3446, 2680, 1695, 1655, 1529, 1504, 1336, 1153,1022cm⁻¹; [α]_(D) ²⁴+20.2±0.6°(c=1.000, MeOH) Anal.(C₂₅H₃₁NO₅S₃.0.3H₂O)Calcd.(%): C, 56.96; H, 6.04; N, 2.66; S, 18.25 Found(%):C, 57.07; H,6.12; N, 2.72; S, 17.88 II-7I-55a ¹H-NMR(CDCl₃) δ 0.91(1H, d, J=10.5Hz),1.09 and 1.22(3H, s), 1.22–2.40(12H, m), 2.39(3H, s), 4.20(1H, m),5.79(1H, br d, J=15.6Hz), 5.99(1H, m), 6.06(1H, d, J=9.0Hz), 6.20(1H, t,J=3.6Hz), 7.03(1H, dt, J= 6.9, 15.6Hz), 7.19(1H, dd, J=1.8, 3.3Hz),7.29(1H, d, J=3.9Hz), 7.55(1H, d, J=3.9Hz); IR(CHCl₃) 3448, 1695, 1655,1529, 1504, 1375, 1182, 1161, 1144, 1053cm⁻¹; [α]_(D)²⁵+19.7±0.6°(c=1.007, MeOH) Anal. (C₂₆H₃₄N₂O₅S₂.0.2H₂O) Calcd.(%): C,59.79; H, 6.64; N, 5.36; S, 12.28 Found(%): C, 59.83; H, 6.40; N, 5.42;S, 12.10. II-7I-55b ¹H-NMR(CDCl₃) δ 0.91(1H, d, J=9.9Hz), 1.09 and 1.22(3H, s), 1.27–1.78(8H, m), 1.99–2.38(6H, m), 2.39(3H, s), 3.72(3H, s),4.19(1H, m), 5.79(1H, dt, J=15.6, 1.5Hz), 5.98(1H, m), 6.03(1H, d,J=9.0Hz), 6.20(1H, t, J= 3.3Hz), 6.93(1H, dt, J=15.6, 6.9Hz), 7.19(1H,dd, J= 1.8, 3.3Hz), 7.28(1H, d, J=3.9Hz), 7.55(1H, d, J= 3.9Hz).II-7I-59a mp 143–145° C.; ¹H-NMR(CDCl₃) δ 0.90(1H, d, J=10.2Hz), 1.08and 1.21(3H, s), 1.24–2.40(14H, m), 4.18(1H, m), 5.79(1H, br d,J=15.6Hz), 5.91(1H, d, J=9.0Hz), 6.98–7.08(3H, m), 7.26(1H, d, J=3.6Hz),7.29(1H, dd, J=1.2, 3.6Hz), 7.42(1H, dd, J=1.2, 5.4Hz); IR(Nujol) 3419,3184, 1705, 1670, 1626, 1525, 1500, 1180cm⁻¹; [α]_(D)²⁶+12.7±0.6°(c=1.007%, MeOH) Anal.(C₂₅H₃₁NO₃S₃) Calcd.(%): C, 61.31; H,6.38; N, 2.86; S, 19.64 Found(%): C, 61.11; H, 6.41; N, 2.92; S, 19.42II-7I-88a ¹H-NMR(CDCl₃) δ 0.91(1H, d, J=10.2Hz), 1.09(3H, s), 1.21(3H,s), 1.26–2.34(14H, m), 4.15(2H, s), 4.20(1H, m), 5.79(1H, dt, J=15.6,1.2Hz), 5.94(1H, d, J=9.3Hz), 6.79(1H, d, J=3.6Hz), 6.97(1H, dd, J=4.8,1.5Hz), 7.05(1H, m), 7.25–7.33(3H, m); IR(CHCl₃) 3523, 3450, 3431, 2679,1695, 1647, 1545, 1506, 1471cm⁻¹; [α]_(D) ^(26.5)+12.7±0.5°(c=1.002,MeOH) Anal. (C₂₆H₃₃NO₃S₂.0.4H₂O) Calcd.(%): C, 65.21; H, 6.92; N, 3.92;S, 13.39 Found(%): C, 65.16; H, 6.63; N, 3.76; S, 13.48

TABLE 54 Compd. No.. Physical property II-7I-104a ¹H-NMR(CDCl₃) δ0.92(1H, d, J=10.2Hz), 1.10(3H, s), 1.22(3H, s), 1.28–2.36(14H, m),4.10(2H, s), 4.21(1H, m), 5.79(1H, dt, J=15.9, 1.5Hz), 5.96(1H, d,J=9.0Hz), 6.70(1H, d, J=3.6Hz), 6.95(1H, dd, J=5.1, 3.6Hz), 7.03(1H, dt,J=15.9, 3.6Hz), 7.04(1H, dd, J=3.6, 1.2Hz), 7.25(1H, d, J=3.6Hz),7.37(1H, dd, J=5.1, 1.2Hz); IR(CHCl₃) 3523, 3450, 3431, 2679, 1695,1649, 1543, 1506cm⁻¹; [α]_(D) ^(25.0)+11.0±0.7°(c=0.709, MeOH)Anal.(C₂₆H₃₃NO₃S₃.0.5H₂O) Calcd.(%): C, 60.99; H, 6.68; N, 2.73; S,19.06 Found(%): C, 60.69; H, 6.45; N, 3.12; S, 19.32 II-7I-126a¹H-NMR(CDCl₃) δ 0.90(1H, d, J=10.2Hz), 1.08(3H, s), 1.21(3H, s),1.27–2.31(14H, m), 3.83(3H, s), 4.12(2H, m), 4.20(1H, m), 5.79(1H, dt,J=15.6, 1.5Hz), 5.92 (1H, d, J=9.3Hz), 6.77(1H, d, J=3.6Hz), 6.86–6.92(2H, m), 7.02(1H, dt, J=15.6, 6.9Hz), 7.16(1H, d, J= 7.5Hz), 7.22(1H,dd, J=7.5, 1.8Hz), 7.27(1H, d, J= 3.6Hz); IR(CHCl₃) 3451, 3433, 2679,1695, 1647, 1504, 1288, 1248, 1223, 1213cm⁻¹; [α]_(D)^(27.0)+14.0±0.5°(c=1.001, MeOH) Anal.(C₂₉H₃₇NO₄S.0.2H₂O) Calcd.(%): C,69.76; H, 7.55; N, 2.81; S, 6.42 Found(%): C, 69.50; H, 7.50; N, 2.88;S, 6.36 II-7I-197a ¹H-NMR(CDCl₃) δ 0.90(1H, d, J=10.2Hz), 1.08(3H, s),1.20(3H, s), 1.26–2.36(14H, m), 3.22(2H, t, J=8.7Hz), 4.07(2H, s),4.19(1H, m), 4.57(2H, t, J=8.7Hz), 5.79 (1H, dt, J=15.6Hz, 1.5Hz),5.92(1H, d, J=9.0Hz), 6.79(1H, t, J=7.2Hz), 6.80(1H, d, J=3.6Hz), 6.96(1H, d, J=7.2Hz), 7.01(1H, dt, J=15.6, 6.9Hz), 7.10 (1H, dd, J=7.2,1.5Hz), 7.29(1H, d, J=3.6Hz); IR (CHCl₃) 3525, 3450, 3431, 2679, 1695,1647, 1543, 1506, 1458cm⁻¹; [α]_(D) ^(25.0)+13.0±0.5°(c=1.002, MeOH)Anal. (C₃₀H₃₇NO₄S.0.2H₂O) Calcd.(%): C, 70.47; H, 7.37; N, 2.74; S, 6.27Found(%): C, 70.48; H, 7.33; N, 2.74; S, 6.29 II-7I-239a mp 138–140° C.;¹H-NMR(CDCl₃) δ 0.87(1H, d, J=10.2Hz), 1.07(3H, s), 1.19(3H, s),1.26–2.31(12H, m), 4.09 (2H, s), 4.20(1H, m), 5.73(1H, d, J=15.6Hz),6.08(1H, d, J=9.0Hz), 6.79(1H, d, J=3.6Hz), 6.81–6.86(2H, m), 6.96(1H,dt, J=15.6, 6.9Hz), 7.29(1H, d, J=3.6Hz), 7.45(1H, s); IR(CHCl₃) 3342,3246, 1720, 1701, 1593, 1545, 1520, 1456, 1377, 1203cm⁻¹; [α]_(D)^(25.0)+13.8±0.5° (c=1.011, MeOH) Anal.(C₃₀H₃₅NO₅S) Calcd.(%): C, 69.07;H, 6.76; N, 2.68; S, 6.15 Found(%): C, 68.91; H, 6.77; N, 2.75; S, 5.99

TABLE 54 Compd. No.. Physical property II-7I-270a ¹H-NMR(CDCl₃) δ0.91(1H, d, J=10.5Hz), 1.09(3H, s), 1.23(3H, s), 1.26–1.55(6H, m),1.62–1.82(2H, m), 1.96–2.38 (6H, m), 2.42(6H, s), 4.20(1H, m), 5.79(1H,dt, J= 15.6, 1.5Hz), 5.88(2H, s), 6.06(1H, d, J=9.0Hz), 7.03 (1H, dt,J=15.6, 6.6Hz), 7.27(1H, d, J=3.9Hz), 7.50 (1H, d, J=3.9Hz); IR(CHCl₃)3525, 3448, 2679, 1695, 1655, 1529, 1504, 1375, 1180, 1119cm⁻¹; [α]_(D)²⁵+19.4±0.6° (c=1.008, MeOH) Anal.(C₂₇H₃₆N₂O₅S₂.0.2H₂O) Calcd.(%): C,60.47; H, 6.84; N, 5.22; S, 11.96 Found(%): C, 60.41; H, 6.77; N, 5.25;S, 11.90 II-7I-327a ¹H-NMR(CDCl₃) δ 0.90(1H, d, J=10.5Hz), 1.07 and 1.21(3H, s), 1.25–2.38(12H, m), 3.00(2H, t, J=8.4Hz), 3.99 (2H, t, J=8.4Hz),4.17(1H, m), 5.78(1H, dt, J=1.8, 15.9Hz), 6.02(1H, d, J=8.7Hz),6.97–7.24(4H, m), 7.27(1H, d, J=4.2Hz), 7.47(1H, d, J=4.2Hz), 7.58(1H,d, J=8.1Hz); IR(CHCl₃) 2927, 1695, 1653, 1529, 1504, 1479, 1367,1165cm⁻¹; [α]_(D) ²⁶+21.3±0.6°(c=1.008%, MeOH); Anal.(C₂₉H₃₆N₂O₅S₂.0.4H₂O) Calcd.(%) C, 61.76; H, 6.58; N, 4.97; S, 11.37Found(%) C, 61.68; H, 6.43; N, 5.02; S, 11.40 II-7I-332a ¹H-NMR(CDCl₃) δ0.91(1H, d, J=10.2Hz), 1.07 and 1.22 (3H, s), 1.30–2.40(16H, m),2.54(2H, t, J=7.2Hz), 3.84–3.89 (2H, m), 4.19(1H, m), 5.79(1H, br d,J=14.4Hz), 6.01(1H, d, J=8.7Hz), 6.97–7.27(5H, m), 7.78(1H, d, J=8.4Hz); IR(CHCl₃) 2929, 1695, 1653, 1529, 1502, 1363, 1211, 1161cm⁻¹;[α]_(D) ²⁴+19.4±0.6°(c=1.010%, MeOH); Anal.(C₃₀H₃₈N₂O₅S₂.0.3H₂O)Calcd.(%) C, 62.54; H, 6.75; N, 4.86; S, 11.13 Found(%) C, 62.56; H,6.76; N, 4.87; S, 10.90 II-7I-343a ¹H-NMR(CDCl₃) δ 0.94(1H, d,J=10.2Hz), 1.11(3H, s), 1.22(3H, s), 1.39–2.39(14H, m), 4.29(1H, m),5.78(1H, d, J=15.6Hz), 6.15(1H, d, J=9.0Hz), 7.02(1H, m), 7.44–7.64 (4H,m), 7.85(1H, s), 8.02–8.12(3H, m), 8.65(1H, d, J= 6.9Hz); IR(CHCl₃)3523, 3444, 2925, 2862, 1695, 1653, 1516, 1493, 1471, 1446, 1419, 1383,1315cm⁻¹; [α]_(D) ^(25.0)+ 34.8±0.7°(c=1.03, MeOH)Anal.(C₃₁H₃₅NO₅S₂.0.4H₂O) Calcd.(%): C, 64.99; H, 6.30; N, 2.44; S,11.19 Found(%): C, 64.97; H, 6.26; N, 2.62; S, 10.86 II-7I-389a mp119–121° C.; ¹H-NMR(CDCl₃) δ 0.90(1H, d, J=10.5Hz), 1.09(3H, s),1.21(3H, s), 1.33–1.50(6H, m), 1.63–1.78 (2H, m), 1.98(1H, m), 2.18(1H,m), 2.23(3H, s), 2.12–2.32(5H, m), 3.21(2H, t, J=8.7Hz), 4.18(1H, m),4.62(2H, t, J=8.7Hz), 5.79(1H, d, J=15.6Hz), 5.95(1H, d, J=9.3Hz),6.90(1H, s), 6.95(1H, s), 7.02(1H, dd, J= 15.6, 6.9Hz), 7.09(1H, d,J=3.6Hz), 7.30(1H, d, J=3.6Hz); IR(Nujol) 3361, 2671, 1695, 1649, 1604,1583, 1533, 1504, 1415, 1323, 1203cm⁻¹; [α]_(D) ²⁵+9.7±0.5°(c=1.012,MeOH) Anal.(C₃₀H₃₇NO₄S₂.0.1H₂O) Calcd.(%): C, 66.54; H, 6.92; N, 2.59;S, 11.84 Found(%): C, 66.42; H, 6.99; N, 2.52; S, 11.92

TABLE 55 Compd. No.. Physical property II-7I-391a ¹H-NMR(CDCl₃) δ0.91(1H, d, J=10.5Hz), 1.09(3H, s), 1.22(3H, s), 1.33–1.52(6H, m),1.67–1.77(2H, m), 2.00(1H, m), 2.12(1H, m), 2.18–2.25(3H, m), 2.32(3H,s)+2.32(1H, m), 3.19(2H, t, J=8.7Hz), 4.20(1H, m), 4.73(2H, t, J=8.7Hz),5.79(1H, dt, J=15.6, 1.5Hz), 6.89(1H, d, J=9.0Hz), 7.03(1H, dt, J=15.6,7.1Hz), 7.21(1H, s), 7.35(1H, d, J= 3.9Hz), 7.51(1H, s), 7.74(1H, d,J=3.9Hz); IR(CHCl₃) 3523, 3448, 2681, 1695, 1652, 1527, 1502, 1481,1329cm⁻¹; [α]_(D) ²⁵+17.1±0.6°(c=1.016, MeOH) Anal. (C₃₀H₃₇NO₆S₂.0.5H₂O)Calcd.(%): C, 62.04; H, 6.60; N, 2.41; S, 11.07 Found(%): C, 62.16; H,6.52; N, 2.37; S, 10.85 II-7J-55a ¹H-NMR(CDCl₃) δ 0.91(1H, d, J=10.2Hz),1.08(3H, s), 1.22(3H, s), 1.24–2.34(14H, m), 1.78(3H, d, J=1.2Hz), 2.38(3H, d, J=1.2Hz), 4.19(1H, s), 5.98(1H, m), 6.04(1H, d, J= 9.0Hz),6.19(1H, t, J=3.3Hz), 6.85(1H, dt, J=7.2, 1.2Hz), 7.19(1H, dd, J=3.3Hz,1.2Hz), 7.28(1H, d, J=3.9Hz), 7.55(1H, d, J=3.9Hz); IR(CHCl₃) 3525,3446, 2667, 1685, 1657, 1529, 1504, 1375, 1281, 1182, 1161, 1053cm⁻¹;[α]_(D) ^(24.0)+ 11.5±0.5°(c=1.000, MeOH) Anal.(C₂₇H₃₆N₂O₅S₂.0.4H₂O)Calcd.(%): C, 60.06; H, 6.87; N, 5.19; S, 11.67 Found(%): C, 60.15; H,6.56; N, 5.00; S, 11.37 II-7K-55a ¹H-NMR(CDCl₃) δ 0.92(1H, d, J=10.5Hz),1.08(3H, s), 1.22(3H, s), 1.24–2.40(14H, m), 2.12(3H, d, J=1.2Hz), 2.39(3H, d, J=1.2Hz), 4.20(2H, s), 5.64(1H, d, J=1.2Hz), 5.99 (1H, m),6.04(1H, d, J=9.0Hz), 6.20(1H, t, J=3.3Hz), 7.19 (1H, dd, J=3.3, 1.8Hz),7.28(1H, d, J=4.2Hz), 7.55(1H, d, J=4.2Hz); IR(CHCl₃) 3523, 3446, 2575;1689, 1655, 1530, 1504, 1375, 1182, 1161, 1053, 1022cm⁻¹; [α]_(D)^(26.5)+18.3±0.6° (c=1.009, MeOH) Anal.(C₂₇H₃₆N₂O₅S₂.0.3H₂O) Calcd.(%):C, 60.27; H, 6.86; N, 5.20; S, 11.92 Found(%): C, 60.23; H, 6.66; N,5.17; S, 11.73 II-7L-55a ¹H-NMR(CDCl₃) δ 0.90(1H, d, J=10.2Hz), 1.00(3H,s), 1.22(3H, s), 1.26–2.61(14H, m), 2.39(3H, s), 4.18(1H, m),5.95–6.08(2H, m), 6.16–6.21(2H, m), 7.19(1H, m), 7.32(1H, d, J=4.2Hz),7.55(1H, d, J=4.2Hz); IR(CHCl₃) 3510, 3446, 2927, 2862, 1709, 1658,1529, 1504, 1441, 1375cm⁻¹; [α]_(D) ^(25.0)+18.4±0.6°(c=1.00, MeOH)Anal. (C₂₆H₃₃FN₂O₅S₂.0.5H₂O) Calcd.(%): C, 57.23; H, 6.28; N, 5.13; F,3.48; S, 11.75 Found(%): C, 57.44; H, 6.31; N, 5.10; F, 3.28; S, 11.27II-7M-1a ¹H-NMR(CDCl₃) δ 0.92(1H, d, J=10.2Hz), 1.09 and 1.23 (3H, s),1.35–2.40(12H, m), 3.54(2H, t, J=6.0Hz), 4.04(2H, s), 4.21(1H, m),6.10(1H, d, J=9.6Hz), 6.32–6.35(2H, m), 7.15–7.18(2H, m), 7.29(1H, d,J=3.9Hz), 7.57(1H, d, J= 3.9Hz); IR(CHCl₃) 3446, 3431, 1780, 1732, 1657,1529, 1504, 1456, 1385, 1192, 1167, 1124, 1057, 1034cm⁻¹; [α]D^(25.5)+22.0±0.6°(c=1.000, MeOH) Anal.(C₂₄H₃₂N₂O₆S₂.0.3H₂O) Calcd.(%): C, 56.08H, 6.39; N, 5.45; S, 12.48 Found(%):C, 56.19; H, 6.39; N, 5.48; S, 12.33

TABLE 56 Compd. No.. Physical property II-7M-1e ¹H-NMR(CDCl₃) δ 0.92(1H,d, J=10.2Hz), 1.10(3H, s), 1.23(3H, s), 1.26–2.34(12H, m), 3.32(3H, s),3.51(2H, d, J= 6.3Hz), 3.99(2H, s), 4.20(1H, m), 6.11(1H, d, J=9.3Hz),6.34(2H, m), 7.17(2H, m), 7.29(1H, d, J=3.9Hz), 7.58(1H, d, J=3.9Hz),8.90(1H, s); IR(CHCl₃) 3448, 3352, 2925, 2870, 1730, 1657, 1529, 1504,1471, 1456, 1423, 1402, 1387, 1354, 1167, 1151, 1120, 1057, 1034cm⁻¹;[α]_(D) ²⁶ +18.7±1.1°(c=0.52, MeOH) Anal. (C₂₅H₃₅N₃O₇S₃.0.7MeOH)Calcd.(%): C, 50.75; H, 6.26; N, 6.91; S, 15.82 Found(%): C, 50.76; H,5.68; N, 6.94; S, 15.49 II-7M-1k ¹H-NMR(CDCl₃) δ 0.93(1H, d, J=10.2Hz),1.11(3H, s), 1.23(3H, s), 1.39–2.33(12H, m), 3.46(2H, t, J=6.6Hz),3.85(2H, s), 4.22(1H, m), 6.12(1H, d, J=9.0Hz), 6.33 (2H, m), 7.15(2H,m), 7.29(1H, m), 7.52–7.66(4H, m), 8.09 (2H, d, J=7.8Hz), 9.03(1H, s);IR(CHCl₃) 3446, 3350, 2924, 2870, 1732, 1657, 1529, 1504, 1473, 1450,1415, 1385, 1167, 1120, 1088, 1057, 1034cm⁻¹; [α]_(D) ²⁶+14.9±0.6°(c=1.00, MeOH) Anal.(C₃₀H₃₇N₃O₇S₃.0.6H₂O) Calcd.(%): C, 54.71; H, 5.85;N, 6.38; S, 14.61 Found(%): C, 54.81; H, 5.76; N, 6.60; S, 14.29II-7M-31a ¹H-NMR(CDCl₃) δ 0.92(1H, d, J=10.2Hz), 1.09 and 1.21 (3H, s),1.39–2.37(12H, m), 3.52(2H, t, J=6.3Hz), 4.03 and 4.14(2H, s), 4.23(1H,m), 6.00(1H, d, J=8.4Hz), 6.77(1H, d, J=3.6Hz), 7.20–7.37(6H, m);IR(CHCl₃) 2923, 1780, 1732, 1641, 1545, 1508, 1471, 1456, 1365, 1248,1219, 1211, 1207, 1124cm⁻¹; [α]_(D) ²⁵+14.9±1.1° (c=0.509%, MeOH);Anal.(C₂₇H₃₅NO₄S₂.0.3H₂O) Calcd.(%) C, 68.27; H, 7.55; N, 2.95; S, 6.75Found(%) C, 68.25; H, 7.62; N, 3.02; S, 6.76 II-7M-40a ¹H-NMR(CDCl₃) δ0.94(1H, d, J=10.2Hz), 1.15 and 1.25 (3H, s), 1.21–2.38(12H, m),3.54(2H, t, J=6.3Hz), 4.05 (2H, s), 4.28(1H, m), 6.11(1H, d, J=9.0Hz),7.25–7.64 (7H, m); IR(CHCl₃) 2924, 1780, 1732, 1641, 1541, 1510, 1491,1471, 1454, 1219, 1211cm⁻¹; [α]_(D) ²⁵+15.7±0.6° (c=1.010%, MeOH);Anal.(C₂₆H₃₃NO₄S.0.3H₂O) Calcd.(%) C, 67.74; H, 7.35; N, 3.04; S, 6.96Found(%) C, 67.68; H, 7.26; N, 3.107; S, 6.75 II-7M-43a mp 95–97° C.;¹H-NMR(CDCl₃) δ 0.94(1H, d, J=10.2Hz), 1.14 and 1.24(3H, s),1.24–2.38(12H, m), 3.54(2H, t, J= 6.3Hz), 4.05(2H, s), 4.27(1H, m),6.07(1H, d, J=8.7Hz), 7.04(1H, dd, J=3.9, 4.8Hz), 7.11(1H, d, J=3.9Hz),7.24 (1H, dd, J=1.2, 3.6Hz), 7.28(1H, dd, J=1.2, 5.1Hz), 7.37 (1H, d,3.9Hz); IR(Nujol) 3346, 2927, 1759, 1728, 1612, 1525, 1504, 1458, 1377,1132cm⁻¹; [α]_(D) ²⁶+18.7±0.6° (c=1.011%, MeOH);Anal.(C₂₄H₃₁NO₄S₂.0.8H₂O) Calcd.(%) C, 60.55; H, 6.90; N, 2.94; S, 13.47Found(%) C, 60.35; H, 6.61; N, 3.07; S, 13.43

TABLE 57 Compd. No.. Physical property II-7M-47a ¹H-NMR(CDCl₃) δ0.91(1H, d, J=10.5Hz), 1.10 and 1.22 (3H, s), 1.36–2.40(12H, m),3.53(2H, t, J=6.0Hz), 4.05 (2H, s), 4.21(1H, m), 6.14(1H, d, J=9.3Hz),7.12(1H, dd, J=0.9, 4.8Hz), 7.35(1H, d, J=3.9Hz), 7.64(1H, d, J= 3.9Hz),7.70(1H, dd, J=1.2, 5.1Hz), 7.76(1H, dd, J=1.2, 3.9Hz); IR(CHCl₃) 3446,3429, 1780, 1732, 1655, 1529, 1504, 1336, 1153, 1124, 1074, 1024cm⁻¹;[α]_(D) ²⁴+22.5±0.6° (c=1.013, MeOH) Anal.(C₂₄H₃₁NO₆S₃.0.4H₂O)Calcd.(%): C, 54.09 H, 6.01; N, 2.63; S, 18.05 Found(%): C, 54.29; H,5.90; N, 2.81; S, 17.77 II-7M-55a ¹H-NMR(CDCl₃) δ 0.92(1H, d, J=10.2Hz),1.09 and 1.23 (3H, s), 1.35–2.40(12H, m), 2.39(3H, s), 3.53(2H, t,J=6.3Hz), 4.04(2H, s), 4.21(1H, m), 5.99(1H, m), 6.12(1H, d, J= 9.6Hz),6.20(1H, t, J=3.3Hz), 7.19(1H, dd, J=1.5, 3.3Hz), 7.32(1H, d, J=3.9Hz),7.55(1H, d, J=3.9Hz); I IR (CHCl₃) 3446, 1780, 1731, 1656, 1529, 1504,1375, 1182, 1161, 1142, 1053cm⁻¹; [α]_(D) ²⁴+20.9±0.6°(c=1.005, MeOH)Anal.(C₂₅H₃₄N₂O₆S₂.0.3H₂O) Calcd.(%): C, 56.86 H, 6.60; N, 5.30; S,12.14 Found(%):, 56.88; H, 6.60; N, 5.31; S, 11.76 II-7M-59a¹H-NMR(CDCl₃) δ 0.91(1H, d, J=10.2Hz), 1.09 and 1.22 (3H, s),1.36–2.38(12H, m), 3.53(2H, t, J=6.0Hz), 4.04 (2H, s), 4.21(1H, m),5.98(1H, d, J=8.7Hz), 7.01(1H, dd, J=3.6, 5.4Hz), 7.05(1H, d, J=3.9Hz),7.27(1H, d, J= 4.2Hz), 7.29(1H, dd, J=1.2, 3.6Hz), 7.43(1H, dd, J=1.5,5.4Hz); IR(CHCl₃) 3448, 3429, 1780, 1732, 1645, 1529, 1500, 1471, 1458,1124cm⁻¹; [α]_(D) ²⁶+17.1±0.9°(c=0.608%, MeOH) Anal.(C₂₄H₃₁NO₄S₃.0.3H₂O)Calcd.(%): C, 57.75 H, 6.38; N, 2.81; S, 19.27 Found(%): C, 57.86; H,6.39; N, 2.89; S, 19.18 II-7M-88a ¹H-NMR(CDCl₃) δ 0.92(1H, d, J=10.2Hz),1.11 and 1.22 (3H, s), 1.42–2.38(12H, m), 3.53(2H, t, J=6.0Hz), 4.03 and4.16(2H, s), 4.24(1H, m), 6.01(1H, d, J=9.0Hz), 6.79(1H, d, J=2.7Hz),6.96(1H, dd, J=1.2, 5.1Hz), 7.05 (1H, m), 7.26–7.33(2H, m); IR(CHCl₃)2924, 1780, 1732, 1641, 1545, 1508, 1471, 1221, 1219, 1211, 1207,1124cm⁻¹; [α]_(D) ²⁵+15.5±1.1°(c=0.505%, MeOH); Anal.(C₂₅H₃₃NO₄S₂.0.3H₂O) Calcd.(%) C, 62.42; H, 7.04; N, 2.91; S, 13.33Found(%) C, 62.57; H, 7.03; N, 2.98; S, 13.15 II-7M- ¹H-NMR(CDCl₃) δ0.91(1H, d, J=10.2Hz), 1.09(3H, s), 126a 1.21(3H, s), 1.45–2.33(12H, m),3.51(2H, t, J=6.3Hz), 3.84(3H, s), 4.02(2H, s), 4.11(2H, s), 4.22(1H,m), 5.99 (1H, d, J=9.0Hz), 6.77(1H, d, J=3.9Hz), 6.86–6.92(2H, m),7.15(1H, dd, J=7.2, 1.8Hz), 7.22(1H, dd, J=4.8, 1.8Hz), 7.29(1H, d,J=3.9Hz); IR(CHCl₃) 3431, 1669, 1506, 1463, 1247, 1128cm⁻¹; [α]_(D)^(27.0)+14.4±0.5°(c=1.009, MeOH) Anal.(C₂₈H₃₇NO₅S.0.2H₂O) Calcd.(%): C,66.82; H, 7.49; N, 2.78; S, 6.37 Found(%): C, 66.59; H, 7.41; N, 2.82;S, 6.17

TABLE 58 Compd. No.. Physical property II-7M-197a ¹H-NMR(CDCl₃) δ0.92(1H, d, J=10.2Hz), 1.10 and 1.21(3H, s), 1.39–2.38(12H, m), 3.22(2H,t, J=9.0Hz), 3.52(2H, t, J=6.3Hz), 4.02 and 4,07(2H, s), 4.23(1H, m),4.58(2H, t, J=9.0Hz), 6.00(1H, d, J=8.4Hz), 6.80–7.12(4H, m), 7.30(1H,d, J=3.6Hz); IR(CHCl₃) 2923, 1780, 1732, 1639, 1545, 1506, 1477, 1458,1441, 1365, 1254, 1205, 1126cm⁻¹; [α]_(D) ²⁶+13.4±1.1° (c=0.506%, MeOH);Anal.(C₂₉H₃₇NO₅S.0.4H₂O) Calcd.(%) C, 67.13; H, 7.34; N, 2.70; S, 6.18Found(%) C, 67.19; H, 7.21; N, 2.75; S, 6.18 II-7M-239a mp 179–180° C.;¹H-NMR(d₆-DMSO) δ 0.78(1H, d, J=9.6Hz), 1.05(3H, s), 1.13(3H, s),1.20–2.30(12H, m), 3.40(2H, t, J=6.3Hz), 3.84(1H, m), 3.93(2H, s),4.17(2H, s), 6.73(1H, dd, J=8.7, 2.4Hz), 6.79(1H, d, J= 2.4Hz), 6.95(1H,d, J=3.6Hz), 7.34(1H, d, J=8.7Hz), 7.66(1H, d, J=3.6Hz), 7.79(1H, d,J=6.9Hz), 7.82(1H, s); IR(KBr) 3338, 3244, 2602, 1739, 1606, 1557, 1550,1525, 1458, 1367, 1261, 1211cm⁻¹; [α]_(D) ^(25.0+) 14.0±0.5°(c=1.009,MeOH) Anal.(C₂₉H₃₅NO₆.0.3H₂O) Calcd.(%): C, 65.59; H, 6.76; N, 2.36; S,6.04 Found(%): C, 65.62; H, 6.82; N, 2.81; S, 5.92 II-7M-270amp.147–149° C.; ¹H-NMR(CDCl₃) δ 0.92(1H, d, J=10.2Hz), 1.09(3H, s),1.23(3H, s), 1.34–2.38(12H, m), 2.42 (6H, s), 3.54(2H, t, J=6.3Hz),4.05(2H, s), 4.21(1H, m), 5.88(2H, s), 6.12(1H, d, J=9.0Hz), 7.28(1H, d,J= 3.9Hz), 7.49(1H, d, J=3.9Hz); IR(Nujol) 3267, 3099, 2549, 1726, 1610,1562, 1230, 1211, 1176, 1126, 1113cm⁻¹; [α]_(D) ²⁶+19.8±0.6°(c=1.010,MeOH) Anal. (C₂₆H₃₆N₂O₆S₂) Calcd.(%): C, 58.18; H, 6.76; N, 5.22; S,11.95 Found(%): C, 58.05; H, 6.74; N, 5.16; S, 11.71 II-7M-307a¹H-NMR(CDCl₃) δ 0.90(1H, d, J=10.5Hz), 1.06(3H, s), 1.19(3H, s),1.38–1.79(8H, m), 1.96(1H, m), 2.06(1H, m), 2.15–2.31(2H, m), 3.49(2H,t, J=6.6Hz), 3.99(3H, s), 4.20(1H, m), 4.60(2H, s), 5.95(1H, d,J=9.0Hz), 6.74(1H, brd, J=3.6Hz), 7.22(1H, d, J=3.6Hz), 7.32 (1H, d,J=9.3Hz), 7.34(1H, ddd, J=1.5, 6.9, 8.4Hz), 7.47(1H, ddd, J=1.5, 6.9,8.4Hz), 7.80(1H, brd, J=8.4Hz), 7.82(1H, d, J=9.3Hz), 7.93(1H, brd,J=8.4Hz); IR(Nujol) 3450, 3060, 1780, 1732, 1639, 1597, 1510, 1471,1265, 1252, 1217cm⁻¹; [α]_(D) ²⁶+16.1±0.6°(c=1.005, MeOH)Anal.(C₃₂H₃₉NO₅S.0.4H₂O) Calcd.(%): C, 69.01; H, 7.20; N, 2.51; S, 5.76Found(%): C, 68.97; H, 7.13; N, 2.56; S, 5.62

TABLE 59 Compd. No.. Physical property II-7M-327a ¹H-NMR(CDCl₃) δ0.91(1H, d, J=10.5Hz), 1.07 and 1.21(3H, s), 1.36–2.35(12H, m), 3.01(2H,t, J=8.4Hz), 3.52(2H, t, J=6.6Hz), 3.99(2H, t, J=8.4Hz), 4.03(2H, s),4.19(1H, m), 6.09(1H, d, J=8.7Hz), 6.99–7.24(3H, m), 7.29(1H, d,J=3.9Hz), 7.47(1H, d, J=3.9Hz), 7.58 (1H, d, J=8.1Hz); IR(CHCl₃) 2924,1780, 1732, 1655, 1529, 1504, 1479, 1460, 1367, 1240, 1225, 1213, 1205,1165, 1122, 1105cm⁻¹; [α]_(D) ²⁶+22.2±0.6°(c=1.009%, MeOH);Anal.(C₂₈H₃₆N₂O₆S₂.0.5H₂O) Calcd.(%) C, 59.03; H, 6.55; N, 4.92; S,11.26 Found(%) C, 58.93; H, 6.75; N, 5.14; S, 11.27 II-7M-329a¹H-NMR(CDCl₃) δ 0.91(1H, d, J=10.5Hz), 1.08 and 1.22(3H, s),1.36–2.38(12H, m), 3.04(2H, t, J=8.4Hz), 3.53(2H, t, J=6.3Hz), 4.04(2H,s), 4.04(2H, t, J=8.4Hz), 4.20(1H, m), 6.11(1H, d, J=8.7Hz), 6.75(1H,m), 7.20(1H, m), 7.30(1H, d, J=3.9Hz), 7.37(1H, brd, J= 7.5Hz), 7.49(1H,d, J=3.9Hz); IR(CHCl₃) 2924, 1780, 1732, 1655, 1626, 1529, 1504, 1473,1460, 1369, 1244, 1223, 1213, 1167cm⁻¹; [α]_(D) ²⁶+21.4±0.6°(c=1.009%,MeOH); Anal.(C₂₈H₃₅FN₂O₆S₂.0.4H₂O) Calcd.(%) C, 57.40; H, 6.16; F, 3.24;N, 4.78; S, 10.95 Found(%) C, 57.37; H, 5.82; F, 3.06; N, 4.86; S, 10.80II-7M-330a ¹H-NMR(CDCl₃) δ 0.91(1H, d, J=10.5Hz), 1.08 and 1.22(3H, s),1.36–2.39(12H, m), 2.97(2H, t, J=8.4Hz), 3.53(2H, t, J=6.3Hz), 4.02(2H,t, J=8.7Hz), 4.04(2H, s), 4.19(1H, m), 6.10(1H, d, J=8.4Hz),6.82–6.94(2H, m), 7.44(1H, d, J=3.9Hz), 7.53(1H, dd, J=4.5, 8.7Hz);IR(CHCl₃) 2924, 1780, 1732, 1655, 1529, 1504, 1481, 1367, 1225,1165cm⁻¹; [α]_(D) ²⁶+21.7±0.6° (c=1.008%, MeOH);Anal.(C₂₈H₃₅FN₂O₆S₂.0.5H₂O) Calcd.(%) C, 57.22; H, 6.17; F, 3.23; N,4.77; S, 10.91 Found(%) C, 57.26; H, 6.14; F, 3.19; N, 4.85; S, 10.76II-7M-331a ¹H-NMR(CDCl₃) δ 0.91(1H, d, J=10.5Hz), 1.08 and 1.22(3H, s),1.36–2.38(12H, m), 3.04(2H, t, J=8.4Hz), 3.53(2H, t, J=6.3Hz), 4.04(2H,s), 4.04(2H, t, J=8.4Hz), 4.20(1H, m), 6.11(1H, d, J=8.7Hz), 6.75(1H,m), 7.20(1H, m), 7.30(1H, d, J=3.9Hz), 7.37(1H, brd, J= 7.5Hz), 7.49(1H,d, J=3.9Hz); IR(CHCl₃) 2924, 1780, 1732, 1655, 1606, 1529, 1492, 1369,1261, 1227, 1205, 1165, 1142, 1095cm⁻¹; [α]_(D) ²⁵+21.4±0.6°(c=1.009%,MeOH); Anal.(C₂₈H₃₅FN₂O₆S₂.0.3H₂O) Calcd.(%) C, 57.57; H, 6.14; F, 3.25;N, 4.80; S, 10.98 Found(%) C, 57.28; H, 5.85; F, 3.20; N, 4.86; S, 10.97

TABLE 60 Compd. No.. Physical property II-7M- ¹H-NMR(CDCl₃) δ 0.92(1H,d, J=10.2Hz), 1.08 and 1.23 332a (3H, s), 1.36–2.40(14H, m), 2.55(2H, t,J=6.6Hz), 3.53 (2H, t, J=6.6Hz), 3.84–3.87(2H, m), 4.05(2H, s), 4.20(1H, m), 6.05(1H, d, J=9.0Hz), 7.04–7.27(5H, m), 7.78 (1H, dd, J=0.9,8.1Hz); IR(CHCl₃) 2925, 1780, 1732, 1655, 1529, 1504, 1489, 1363, 1236,1225, 1213, 1207, 1161, 1122cm⁻¹; [α]_(D) ²⁴+19.5±0.6°(c=1.015%, MeOH);Anal.(C₂₉H₃₈N₂O₆S₂.0.4H₂O) Calcd.(%) C, 59.85; H, 6.72; N, 4.81; S,11.02 Found(%) C, 59.84; H, 6.75; N, 4.92; S, 11.16 II-7M- ¹H-NMR(CDCl₃)δ 0.91(1H, d, J=10.2Hz), 1.08 and 1.23 333a (3H, s), 1.36–2.40(12H, m),3.53(2H, t, J=6.3Hz), 3.87–3.96 (4H, m), 4.05(2H, s), 4.20(1H, m),6.09(1H, d, J=9.0Hz), 6.85(1H, dd, J=1.5, 8.4Hz), 6.96(1H, m), 7.11(1H,m), 7.26–7.30(2H, m), 7.83(1H, dd, J=1.5, 8.1Hz); IR (CHCl₃) 2924, 1780,1732, 1655, 1529, 1502, 1491, 1367, 1248, 1215, 1207, 1165, 1126cm⁻¹;[α]_(D) ²⁶+20.5±0.6° (c=1.004%, MeOH); Anal.(C₂₈H₃₆N₂O₇S₂.0.4H₂O)Calcd.(%) C, 57.59; H, 6.35; N, 4.80; S, 10.98 Found(%) C, 57.59; H,6.24; N, 4.89; S, 10.78 II-7M- ¹H-NMR(CDCl₃) δ 0.91(1H, d, J=10.2Hz),1.08 and 1.23 334a (3H, s), 1.36–2.40(12H, m), 3.05(2H, dd, J=5.4,9.0Hz), 3.54(2H, t, J=6.3Hz), 4.03–4.07(4H, m), 4.21(lH, m), 6.07(1H, d,J=8.7Hz), 7.09–7.27(5H, m), 7.67(1H, m); IR (CHCl₃) 2924, 1780, 1732,1655, 1529, 1504, 1473, 1363, 1161cm⁻¹; [α]_(D) ²⁴+24.4±0.6°(c=1.013%,MeOH); Anal. (C₂₈H₃₆N₂O₆S₃.0.4H₂O) Calcd.(%) C, 56.05; H, 6.18; N, 4.67;S, 16.03 Found(%) C, 56.18; H, 6.09; N, 4.69; S, 15.74 II-7M- mp166–168° C.; ¹H-NMR(d6-DMSO) δ 0.79(1H, d, J=9.6Hz), 336a 1.03 and1.22(3H, s), 1.22–1.58(8H, m), 1.91(1H, m), 2.08–2.30(4H, m), 3.39(2H,t, J=6.0Hz), 3.85(1H, m), 3.92(2H, s), 4.63(4H, s), 7.20–7.35(4H, m),7.77(1H, d, J= 3.9Hz), 7.94(1H, d, J=3.9Hz), 8.24(1H, d, J=6.9Hz);IR(Nujol) 3369, 3093, 2924, 1730, 1612, 1541, 1516, 1466, 1377, 1344,1215, 1165, 1126, 1084cm⁻¹; [α]_(D) ²⁵+19.0±0.6° (c=1.003%, MeOH);Anal.(C₂₈H₃₆N₂O₆S₂.0.7H₂O) Calcd.(%) C, 58.66; H, 6.57; N, 4.89; S,11.19 Found(%) C, 58.38; H, 6.40; N, 4.99; S, 11.48 II-7M- ¹H-NMR(CDCl₃)δ 0.94(1H, d, J=10.2Hz), 1.11(3H, s), 343a 1.23(3H, s), 1.44–2.36(12H,m), 3.49(2H, t, J=6.9Hz), 3.99(2H, t, J=6.9Hz), 4.29(1H, m), 6.27(1H, d,J=9.3Hz), 7.44–7.63(4H, m), 7.89(1H, s), 8.01–8.11(3H, m), 8.63 (1H, d,J=7.5Hz); IR(CHCl₃) 3442, 2924, 2870, 1780, 1730, 1653, 1518, 1417,1446, 1383, 1317cm⁻¹; [α]_(D) ^(26.0+) 24.3±0.6°(c=1.01, MeOH)Anal.(C₃₀H₃₅NO₆S₂.1.7H₂O) Calcd.(%): C, 60.02; H, 6.45; N, 2.33; S,10.68 Found(%): C, 60.14; H, 6.18; N, 2.40; S, 10.3

TABLE 61 Compd. No.. Physical property II-7M-385a ¹H-NMR(CDCl₃) δ0.96(1H, d, J=10.2Hz), 1.16(3H, s), 1.23(3H, s), 1.37–2.39(12H, m),3.52(2H, t, J=6.3Hz), 4.02(2H, s), 4.35(1H, m), 6.26(2H, t, J=2.4Hz),6.48 (1H, d, J=7.8Hz), 7.21(2H, t, J=2.4Hz), 7.57–7.59 (2H, m), 8.39(1H,m), 8.44(1H, s); IR(CHCl₃) 3456, 3103, 3022, 2924, 1732, 1651, 1516,1371, 1221, 1188, 1163, 1057cm⁻¹; [α]_(D) ^(22.0)+42.9±0.8°(c=1.008,MeOH) Anal.(C₂₈H₃₄N₂O₆S₂.0.1H₂O) Calcd.(%): C, 60.00; H, 6.15; N, 5.00;S, 11.44 Found(%): C, 59.85; H, 6.29; N, 4.82; S, 11.28 II-7M-389a mp112–114° C.; ¹H-NMR(CDCl₃) δ 0.91(1H, d, J=10.5Hz), 1.09(3H, s),1.21(3H, s), 1.39–1.52(4H, m), 1.59–1.81 (4H, m), 1.98(1H, m), 2.11(1H,m), 2.23(3H, s) + 2.18–2.34(2H, m), 3.21(2H, t, J=8.7Hz), 3.52(2H, t, J=6.5Hz), 4.05(2H, s), 4.20(1H, m), 4.62(2H, t, J=8.7Hz), 6.00(1H, d,J=9.0Hz), 6.90(1H, s), 6.96(1H, s), 7.08(1H, d, J=4.2Hz), 7.32(1H, d,J=4.2Hz); IR (Nujol) 3406, 3338, 2729, 1757, 1738, 1614, 1583, 1533,1503, 1203, 1124cm⁻¹; [α]_(D) ²³+12.2±0.5°(c=1.013, MeOH)Anal.(C₂₉H₃₇NO₅S₂.0.2H₂O) Calcd.(%): C, 63.64; H, 6.89; N, 2.56; S,11.72 Found(%): C, 63.68; H, 6.83; N, 2.55; S, 11.54 II-7M-390a mp120–122° C.; ¹H-NMR(CDCl₃) δ 0.91(1H, d, J=10.2Hz), 1.08(3H, s),1.21(3H, s), 1.38–1.52(4H, m), 1.56–1.78 (4H, m), 1.98(1H, m), 2.10(1H,m), 2.17–2.33(2H, m), 2.39(3H, s), 3.52(2H, t, J=6.3Hz), 4.04(2H, s),4.20(1H, m), 6.00(1H, d, J=9.0Hz), 6.72(1H, d, J=2.1Hz), 7.09(1H, m),7.18(1H, d, J=3.9Hz), 7.33(1H, m) + 7.34(1H, d, J=3.9Hz), 7.63(1H, d,J=2.1Hz) ; IR (CHCl₃) 3508, 3448, 3429, 2667, 2568, 1780, 1732, 1645,1529, 1500, 1471, 1421, 1323, 1246, 1130,cm⁻¹; [α]_(D)²⁴+12.5±0.5°(c=1.008, MeOH) Anal. (C₂₉H₃₅NO₅S₂.0.3H₂O) Calcd.(%): C,63.66; H, 6.56; N, 2.56; S, 11.72 Found(%): C, 63.74; H, 6.44; N, 2.54;S, 11.78 II-7M-391a mp 177–179° C.; ¹H-NMR(CDCl₃) δ 0.91(1H, d,J=10.2Hz), 1.10(3H, s), 1.22(3H, s), 1.40–1.53(4H, m), 1.57–1.71 (3H,m), 1.79(1H, m), 2.00(1H, m), 2.11(1H, m), 2.19–2.35(2H, m)+2.32(3H, s),3.19(2H, t, J=8.7Hz), 3.53(2H, t, J=6.5Hz), 4.05(2H, s), 4.21(1H, m),4.73 (2H, t, J=8.7Hz), 6.17(1H, d, J=9.0Hz), 7.21(1H, s), 7.36(1H, d,J=3.9Hz), 7.51(1H, s), 7.74(1H, d, J=3.9Hz); IR(Nujol) 3249, 2754, 2677,2553, 1736, 1622, 1564, 1331, 1225, 1196, 1155, 1134cm⁻¹; [α]_(D)²⁵+17.1±0.6°(c=1.006, MeOH) Anal. (C₂₉H₃₇NO₇S₂.0.2H₂O) Calcd.(%): C,60.12; H, 6.51; N, 2.42; S, 11.07 Found(%): C, 60.09; H, 6.47; N, 2.32;S, 11.06

TABLE 62 Compd. No.. Physical property II-7M-392a mp 155–156° C.;¹H-NMR(CDCl₃) δ 0.89(1H, d, J=9.9Hz), 1.08(3H, s), 1.20(3H, s),1.36–1.52(4H, m), 1.55–1.69 (3H, m), 1.78(1H, m), 1.99(1H, m), 2.10(1H,m), 2.17–2.34(2H, m), 2.51(3H, s), 3.51(2H, t, J=6.5Hz), 4.04(2H, s),4.19(1H, m), 6.17(1H, d, J=8.7Hz), 6.78 (1H, d, J=2.1Hz), 7.36(1H, d,J=3.9Hz), 7.64(1H, m), 7.75(1H, d, J=2.1Hz), 7.77(1H, m), 7.83(1H, d,J=3.9Hz); IR(Nujol) 3323, 1734, 1624, 1536, 1321, 1153, 1126cm⁻¹;[α]_(D) ²⁵+20.4±0.6°(c=1.006, MeOH) Anal. (C₂₉H₃₅NO₇S₂.0.6H₂O)Calcd.(%): C, 59.59; H, 6.24; N, 2.40; S, 10.97 Found(%): C, 59.57; H,6.12; N, 2.37; S, 10.77 II-7M-393a ¹H-NMR(CDCl₃) δ 0.90(3H, t, J=7.2Hz),0.91(1H, d, J= 9.3Hz), 1.09(3H, s), 1.21(3H, s), 1.25–1.79(12H, m),1.98(1H, m), 2.10(1H, m), 2.17–2.34(2H, m), 2.47(2H, t, J=7.7Hz),3.23(2H, t, J=8.7Hz), 3.52(2H, t, J=6.3Hz), 4.04(2H, s), 4.21(1H, m),4.62(2H, t, J=8.7Hz), 5.99(1H, d, J=9.0Hz), 6.93(1H, s), 6.98(1H, s),7.07 (1H, d, J=3.9Hz), 7.31(1H, d, J=3.9Hz); IR(CHCl₃) 3058, 3448, 3429,1780, 1732, 1643, 1529, 1500, 1466, 1419, 1248, 1124cm⁻¹; [α]_(D)²⁴+12.7±0.5°(c=1.014, MeOH) Anal.(C₃₂H₄₃NO₅S₂.0.2H₂O) Calcd.(%): C,65.21; H, 7.42; N, 2.38; S, 10.88 Found(%): C, 65.09; H, 7.37; N, 2.35;S, 11.02 II-7N-55a ¹H-NMR(CDCl₃) δ 0.92(1H, d, J=10.5Hz), 1.08 and1.23(3H, s), 1.56(1H, ddd, J=2.7, 6.0, 13.5Hz), 1.90–2.46 (7H, m),2.39(3H, s), 4.11(2H, d, J=1.2Hz), 4.14–4.19 (3H, m), 5.57–5.76(2H, m),5.99(1H, m), 6.17–6.21 (2H, m), 7.19(1H, dd, J=1.8, 3.3Hz), 7.34(1H, d,J=3.9Hz), 7.55(1H, d, J=3.9Hz); IR(CHCl₃) 3446, 1732, 1657, 1529, 1504,1375, 1182, 1161, 1142, 1119, 1053cm⁻¹; [α]_(D) ²⁴+40.4±0.8°(c=1.001,MeOH) Anal. (C₂₅H₃₂N₂O₆S₂.0.3H₂O) Calcd.(%): C, 57.08 H, 6.25; N, 5.32;S, 12.19 Found(%): C, 57.07; H, 6.18; N, 5.39; S, 11.91 II-7O-55a¹H-NMR(CDCl₃) δ 0.92(1H, d, J=10.2Hz), 1.09 and 1.23(3H, s), 1.55(1H,ddd, J=2.7, 5.7, 13.5Hz), 1.85–2.40 (7H, m), 2.39(3H, s), 3.93–4.05(4H,m), 4.25(1H, m), 5.58–5.79(2H, m), 6.00(1H, m), 6.11(1H, d, J=9.0Hz),6.20(1H, t, J=3.3Hz), 7.19(1H, dd, J=1.5, 3.3Hz), 7.32(1H, d, J=4.2Hz),7.55(1H, d, J=4.2Hz); IR (CHCl₃) 3444, 1778, 1732, 1657, 1529, 1504,1375, 1182, 1161, 1144, 1053cm⁻¹; [α]_(D) ^(24.5)+15.8±0.6°(c=1.008,MeOH) Anal.(C₂₅H₃₂N₂O₆S₂.0.4H₂O) Calcd.(%): C, 56.88 H, 6.26; N, 5.31;S, 12.15 Found(%): C, 56.91; H, 6.17; N, 5.30; S, 12.14

TABLE 63 Compd. No.. Physical property II-7P-55a ¹H-NMR(CDCl₃) δ0.89(1H, d, J=10.2Hz), 1.09(3H, s), 1.23(3H, s), 1.54(1H, m),1.95–2.35(7H, m), 2.39(3H, s), 4.14–4.31(5H, m), 5.39(1H, dt, J=7.8Hzand 20.7Hz), 5.99(1H, m), 6.20(1H, m), 6.29(1H, d, J=5.4Hz), 7.18 (1H,m), 7.36(1H, d, J=3.9Hz), 7.53(1H, d, J=3.9Hz); IR(CHCl₃) 3446, 2925,1732, 1655, 1531, 1504, 1375, 1161, 1142, 1053, 1022cm⁻¹; [α]_(D)²⁴+30.1±0.7°(c=1.01, MeOH) Anal.(C₂₅H₃₁FN₂O₆S₂.0.7MeOH) Calcd.(%): C,55.01; H, 6.07; N, 4.99; F, 3.39; S, 11.43 Found(%): C, 55.21; H, 5.92;N, 5.11; F, 3.49; S, 11.16 II-7P-55e ¹H-NMR(CDCl₃) δ 0.91(1H, d,J=10.2Hz), 1.10(3H, s), 1.25(3H, s), 1.97–2.37(8H, m), 2.39(3H, s),3.28(3H, s), 3.99–4.28(5H, m), 5.41(1H, dt, J=8.7 and 20.4Hz), 5.99 (1H,m), 6.13(1H, d, J=8.4Hz), 6.20(1H, m), 7.19(1H, m), 7.33(1H, d,J=4.2Hz), 7.55(1H, d, J=4.2Hz); IR (CHCl₃) 3448, 3352, 2925, 1728, 1657,1529, 1504, 1425, 1402, 1375, 1348, 1157, 1053, 1020cm⁻¹; [α]_(D)²⁴+32.7±1.5° (c=0.49, MeOH) Anal.(C₂₆H₃₄FN₃O₇S₃.0.45MeOH) Calcd.(%): C,50.41; H, 5.73; N, 6.67; F, 3.01; S, 15.26 Found(%): C, 50.80; H, 5.81;N, 6.63; F, 2.85; S, 14.87 II-7P-55j ¹H-NMR(CDCl₃) δ 0.90(1H, d,J=10.2Hz), 1.09(3H, s), 1.24(3H, s), 1.51–2.37(8H, m), 2.39(3H, s),3.97(2H, s), 4.17–4.25(3H, m), 5.39(1H, dt, J=9.0 and 20.7Hz), 5.99 (1H,m), 6.20(1H, m), 6.37(1H, d, J=8.1Hz), 6.71(1H, s), 7.19(1H, m),7.39(1H, d, J=3.9Hz), 7.55(1H, d, J=3.9Hz); IR(CHCl₃) 3519, 3402, 2925,2870, 1745, 1689, 1657, 1574, 1529, 1504, 1471, 1448, 1375, 1161, 1144,1092, 1053, 1022cm⁻¹; [α]_(D) ²⁵+40.8±1.6°(c=0.51, MeOH) II-7Q-55a¹H-NMR(CDCl₃) δ 0.90(1H, d, J=10.2Hz), 1.11 and 1.23 (3H, s), 1.53(1H,ddd, J=2.1, 5.7, 13.5Hz), 1.70–2.38(7H, m), 2.38(3H, s), 3.52(2H, t,J=6.3Hz), 3.96–4.13(2H, m), 4.23(1H, m), 5.97–6.04(2H, m), 6.14(1H, d,J=9.3Hz), 6.20(1H, t, J=3.6Hz), 6.96(1H, dt, J=4.2, 15.6Hz), 7.18 (1H,m), 7.27(1H, d, J=3.9Hz), 7.54(1H, d, J=3.9Hz); IR(CHCl₃) 2925, 1701,1657, 1529, 1504, 1375, 1215, 1182, 1161, 1142cm⁻¹; [α]₃₆₅ ²⁶−42.1±0.8°(c=1.001%, MeOH); Anal.(C₂₅H₃₂N₂O₆S₂.0.4H₂O) Calcd.(%) C,56.88; H, 6.26; N, 5.31; S, 12.15 Found(%) C, 56.95; H, 6.11; N, 5.35;S, 12.11 II-7R-55a ¹H-NMR(CDCl₃) δ 0.92(1H, d, J=10.2Hz), 1.09 and 1.22(3H, s), 1.35–2.40(12H, m), 2.39(3H, s), 2.64(2H, t, J=7.2Hz), 3.20(2H,s), 4.20(1H, m), 4.52(1H, brs), 5.99(1H, m), 6.16(1H, d, J=8.7Hz),6.20(1H, t, J=3.3Hz), 7.19 (1H, dd, J=1.8, 3.3Hz), 7.31(1H, d, J=3.9Hz),7.55(1H, d, J=3.9Hz); IR(CHCl₃) 3446, 2675, 2565, 1711, 1657, 1529,1504, 1375, 1182, 1161, 1144, 1053cm⁻¹; [α]_(D) ²⁴⁺ 23.5±0.6°(c=1.007,MeOH) Anal.(C₂₅H₃₄N₂O₅S₃.0.3H₂O) Calcd.(%): C, 55.18; H, 6.41; N, 5.15;S, 17.68 Found(%): C, 55.29; H, 6.31; N, 5.12; S, 17.46

TABLE 64 Compd. No.. Physical property II-7R-88a ¹H-NMR(CDCl₃) δ0.93(1H, d, J=10.2Hz), 1.10 and 1.22(3H, s), 1.36–2.40(12H, m), 2.65(2H,t, J=6.9Hz), 3.17 and 3.22(each 1H, ABq, J=14.7Hz), 4.16(2H, s),4.23(1H, m), 4.60(1H, brs), 6.04(1H, d, J=9.3Hz), 6.79(1H, brd,J=3.9Hz), 6.96(1H, dd, J=1.5, 5.1Hz), 7.05(1H, m), 7.28(1H, dd, J=3.0,4.8Hz), 7.32(1H, d, J= 3.6Hz); IR(CHCl₃) 3450, 3430, 1711, 1641, 1545,1508, 1471, 1460, 1294, 1263, 1126cm⁻¹; [α]_(D) ²⁴⁺ 18.0±0.6°(c=1.003,MeOH) Anal. (C₂₅H₃₃NO₃S₃.0.3H₂O) Calcd.(%): C, 60.40; H, 6.81; N, 2.82;S, 19.35 Found(%): C, 60.42; H, 6.60; N, 2.99; S, 19.47 II-7R-270amp.150–152° C.; ¹H-NMR(CDCl₃) δ 0.92(1H, d, J=10.5Hz), 1.09(3H, s),1.23(3H, s), 1.34–2.38(12H, m), 2.42 (6H, s), 2.64(2H, t, J=7.2Hz),3.20(2H, s), 4.21(1H, m), 5.88(2H, s), 6.15(1H, d, J=9.0Hz), 7.29(1H, d,J= 3.9Hz), 7.49(1H, d, J=3.9Hz); IR(Nujol) 3365, 3084, 1709, 1622, 1549,1367, 1176, 1126cm⁻¹; [α]_(D) ²⁷⁺ 22.7±0.6°(c=1.001, MeOH) Anal.(C₂₆H₃₆N₂O₅S₃.0.2(C₆H₁₄O)) Calcd.(%): C, 57.31; H, 6.86; N, 4.91; S,16.88 Found(%): C, 57.18; H, 6.78; N, 4.89; S, 16.95 II-7S-47a¹H-NMR(CDCl₃) δ 0.86(1H, d, J=10.2Hz), 1.08 and 1.20(each 3H, s),1.38–2.40(10H, m), 3.89–4.20(4H, m), 6.68–6.72(2H, d, m), 7.11(1H, dd,J=3.6, 4.8Hz), 7.44 (1H, d, J=4.2Hz), 7.59(1H, d, J=4.2Hz), 7.71(1H, dd,J=3.6, 5.1Hz), 7.74(1H, dd, J=1.2, 3.9Hz); IR(CHCl₃) 3346, 3097, 1730,1649, 1533, 1506, 1402, 1335, 1153, 1024cm⁻¹; [α]_(D)²⁴+27.5±0.7°(c=1.003, MeOH) Anal. (C₂₄H₃₀N₂O₆S₃.0.5H₂O) Calcd.(%): C,52.63; H, 5.70; N, 5.11; S, 17.56 Found(%): C, 52.45; H, 5.39; N, 5.211;S, 17.62 II-7S-55a mp 99–101° C.; ¹H-NMR(CDCl₃) δ 0.87(1H, d, J=10.2Hz),1.08 and 1.21(each 3H, s), 1.40–2.40(10H, m), 2.38 (3H, s),3.91–4.20(3H, m), 5.99(1H, m), 6.20(1H, t, J= 3.6Hz), 6.53–6.60(2H, d,m), 7.17(1H, dd, J=1.8, 3.3Hz), 7.41(1H, d, J=4.2Hz), 7.53(1H, d,J=4.2Hz); IR (Nujol) 3321, 3089, 1736, 1709, 1660, 1633, 1550, 1377,1236, 1184, 1159, 1051cm⁻¹; [α]_(D) ²⁴+28.5±0.7°(c=1.006, MeOH)Anal.(C₂₅H₃₃N₃O₆S₂) Calcd.(%): C, 56.05; H, 6.21; N, 7.84; S, 11.97Found(%): C, 55.74; H, 6.17; N, 7.71; S, 11.81

TABLE 65 Compd. No.. Physical property II-7T-55a ¹H-NMR(CDCl₃) δ0.86(1H×1/2, d, J=10.5Hz), 0.90 (1H×1/2, d, J=10.5Hz), 1.05, 1.08, 1.20and 1.22(each 3H×1/2, s), 1.40–2.57(10H, m), 2.39(3H, s), 4.18(1H, m),4.47 and 4.57(each 1H×1/2, ABq, J=17.1Hz), 4.49 and 4.59(each 1H×1/2,ABq, J=17.1Hz), 5.99(1H, m), 6.20 (1H, m), 6.36(1H, m), 6.73(1H×1/2, t,J=6.0Hz), 7.18 (1H, m), 7.32(1H×1/2, d, J=3.9Hz), 7.38(1H×1/2, d, J=3.9Hz), 7.46(1H×1/2, t, J=6.0Hz), 7.53(1H, d, J=3.9Hz); IR(CHCl₃) 3446,1765, 1732, 1655, 1531, 1504, 1375, 1182, 1161, 1144, 1053, 1022cm⁻¹;[α]_(D) ²⁵ −4.2±0.4° (c=1.008, MeOH) Anal.(C₂₄H₃₁N₃O₆S₂) Calcd.(%): C,55.26; H, 5.99; N, 8.06; S, 12.29 Found(%): C, 55.20; H, 5.88; N, 7.81;S, 11.94 II-7U-31a ¹H-NMR(CDCl₃) δ 0.91(1H, d, J=10.2Hz), 1.10 and 1.22(3H, s), 1.47(1H, m), 1.64–2.63(12H, m), 4.13(2H, s), 4.20 (1H, m),6.07(1H, d, J=8.4Hz), 6.77(1H, d, J=3.9Hz), 7.22–7.36(6H, m); IR(CHCl₃)2924, 1709, 1643, 1543, 1506, 1471, 1454, 1284, 1223, 1213, 1205cm⁻¹;[α]_(D) ²⁶⁺ 25.1±1.3°(c=0.507%, MeOH); Anal. (C₂₇H₃₅NO₃S₂.0.3H₂O)Calcd.(%) C, 66.03; H, 7.31; N, 2.83; S, 13.06 Found(%) C, 66.03; H,7.37; N, 2.96; S, 13.09 II-7U-55a ¹H-NMR(CDCl₃) δ 0.89(1H, d, J=10.2Hz),1.10 and 1.22 (3H, s), 1.48(1H, ddd, J=2.4, 5.4, 13.2Hz), 1.65–2.60(12H, m), 2.40(3H, s), 4.18(1H, m), 5.99(1H, m), 6.20(1H, t, J=3.3Hz),6.23(1H, d, J=8.4Hz), 7.19(1H, dd, J=1.8, 3.3Hz), 7.33(1H, d, J=4.2Hz),7.55(1H, d, J=4.2Hz); IR(CHCl₃) 2925, 1741, 1709, 1657, 1529, 1504,1375, 1221, 1211, 1207, 1182, 1161, 1144cm⁻¹; [α]_(D) ²⁵+29.1±0.7°(c=1.008%, MeOH); Anal.(C₂₅H₃₄N₂O₅S₃.0.3H₂O) Calcd.(%) C, 55.18; H,6.41; N, 5.15; S, 17.68 Found(%) C, 55.20; H, 6.25; N, 5.21; S, 17.71II-7U-88a ¹H-NMR(CDCl₃) δ 0.91(1H, d, J=10.2Hz), 1.11 and 1.22 (3H, s),1.47(1H, m), 1.64–2.63(12H, m), 4.16(2H, s), 4.21 (1H, m), 6.08(1H, d,J=8.7Hz), 6.79(1H, d, J=3.9Hz), 6.96(1H, dd, J=1.2, 5.1Hz), 7.05(1H, m),7.27–7.34(3H, m); IR(CHCl₃) 2924, 1709, 1643, 1543, 1508, 1471, 1284,1238, 1217cm⁻¹; [α]_(D) ²⁵+24.9±0.6°(c=1.014%, MeOH);Anal.(C₂₅H₃₃NO₃S₃.0.4H₂O) Calcd.(%) C, 60.18; H, 6.83; N, 2.81; S, 19.28Found(%) C, 60.20; H, 6.77; N, 2.94; S, 19.34 II-7V-55a ¹H-NMR(CDCl₃) δ0.92(1H, d, J=10.8Hz), 1.09(3H, s), 1.23(3H, s), 1.26–2.34(14H, m),2.39(3H, s), 4.20(1H, m), 5.99–6.07(2H, m), 6.13–6.29(2H, m), 7.19(1H,m), 7.29 (1H, d, J=3.9Hz), 7.55(1H, d, J=3.9Hz); IR(CHCl₃) 3512, 3446,2927, 2862, 2553, 1711, 1658, 1529, 1504, 1431, 1375, 1279cm⁻¹; [α]_(D)^(26.0)+16.0±1.1°(c=0.50, MeOH)

(C₂₆H₃₃FN₂O₅S₂.0.6MeOH) Calcd.(%): C, 57.47; H, 6.42; N, 5.04; F, 3.42;S, 11.5 Found(%): C, 57.77; H, 6.28; N, 4.95; F, 3.33; S, 11.15

TABLE 66 Compd. No.. Physical property II-8C-55a ¹H-NMR(d₆-DMSO) δ0.77(1H, d, J=9.6Hz), 1.03(3H, s), 1.12(3H, s), 1.13–1.52(9H, m),1.89(1H, m), 2.06–2.30 (4H, m), 2.32(3H, s), 3.39(2H, m), 3.62(2H, s),3.84(1H, m), 6.10(1H, m), 6.27(1H, t, J=3.3Hz), 7.25(1H, dd, J= 3.3,1.5Hz), 7.87(1H, d, J=3.9Hz), 7.98(1H, d, J=3.9Hz), 8.45(1H, d,J=7.2Hz); IR(Nujol) 3332, 1623, 1536, 1457, 1375, 1182, 1160cm⁻¹;[α]_(D) ^(24.0)+15.1±0.6°(c=1.006, DMSO) Anal.(C₂₆H₃₆N₂O₆S₂.2.0H₂O)Calcd.(%): C, 53.52; H, 7.04; N, 4.89; S, 11.10 Found(%): C, 53.38; H,6.74; N, 4.82; S, 10.88 II-8C-88a ¹H-NMR(d₆-DMSO) δ 0.77(1H, d,J=9.3Hz), 1.05(3H, s), 1.13(3H, s), 1.14–1.66(8H, m), 1.86–2.28(6H, m),3.38 (2H, m), 3.60(2H, s), 3.85(1H, m), 4.13(2H, s), 6.88(1H, d,J=3.6Hz), 6.99(1H, dd, J=5.1, 0.9Hz), 7.28(1H, m), 7.48(1H, dd, J=5.1,3.0Hz), 7.67(1H, d, J=3.6Hz), 7.82 (1H, d, J=7.2Hz); IR(Nujol) 3413,1623, 1508, 1459, 1091cm⁻¹; [α]_(D) ^(24.0)+12.6±1.1°(c=0.500, DMSO)Anal. (C₂₆H₃₅NO₄S₂.2.0H₂O) Calcd.(%): C, 58.40; H, 7.28; N, 2.66; S,12.00 Found(%): C, 58.43; H, 7.01; N, 2.73; S, 11.73 VI-6A-1a¹H-NMR(CDCl₃) δ 0.86(1H, m), 1.04–1.66(15H, m), 1.95(1H, m), 2.15(1H,brs), 2.33(2H, t, J=7.5Hz), 3.26 (1H, m), 3.49(1H, m), 6.11(1H, brt),6.33(2H, t, J=2.4Hz), 7.16(2H, t, J=2.4Hz), 7.33 and 7.57(each 1H, eachd, each J=4.2Hz); IR(CHCl₃) 3514, 3446, 2679, 1709, 1658, 1535, 1509,1456, 1385, 1274, 1192, 1192, 1167, 1057, 1034cm⁻¹; [α]_(D)²⁶+8.7±0.5°(c=1.002, MeOH) Anal. (C₂₃H₃₀N₂O₅S₂.0.1H₂O) Calcd.(%): C,57.50; H, 6.34; N, 5.83; S, 13.35 Found(%): C, 57.56; H, 6.46; N, 5.91;S, 13.04 VI-6A-47a ¹H-NMR(CDCl₃) δ 0.87(1H, m), 1.04–1.66(15H, m), 1.95(1H, m), 2.16(1H, brs), 2.33(2H, t, J=7.5Hz), 3.27(1H, m), 3.49(1H, m),6.24(1H, brt), 7.11(1H, dd, J=3.6 and 4.8Hz), 7.39 and 7.63(each 1H,each d, each J=3.9Hz), 7.70(1H, dd, J=1.2 and 4.8Hz), 7.75(1H, dd, J=1.2and 3.6Hz); IR(CHCl₃) 3514, 3446, 1709, 1657, 1533, 1506, 1402, 1336,1153, 1097, 1024cm⁻¹; [α]_(D) ²⁶+7.4±0.5° (c=1.014, MeOH)Anal.(C₂₃H₂₉NO₅S₃.0.4H₂O) Calcd.(%): C, 55.93; H, 5.97; N, 2.79; S,19.13 Found(%): C, 55.08; H, 6.09; N, 2.93; S, 19.03 VI-6A-88a¹H-NMR(CDCl₃) δ 0.87(1H, m), 1.04–1.68(15H, m), 1.94 (1H, m), 2.17(1H,brs), 2.33(2H, t, J=7.5Hz), 3.20(1H, m), 3.53(1H, m), 4.15(2H, s),5.87(1H, brt), 6.78(1H, m), 6.96(1H, dd, J=1.2 and 5.1Hz), 7.05(1H, m),7.28(1H, dd, J=3.0 and 5.1Hz), 7.34(1H, d, J=3.6Hz); IR(CHCl₃) 3516,3452, 1709, 1645, 1547, 1513, 1462cm⁻¹; [α]_(D) ²⁶⁺ 8.4±0.5°(c=1.015,MeOH) Anal.(C₂₄H₃₁NO₃S₂.0.2H₂O) Calcd.(%): C, 64.17; H, 7.04; N, 3.12;S, 14.28 Found(%): C, 64.16; H, 7.13; N, 3.18; S, 14.09

TABLE 67 Compd. No.. Physical property VII-GA-1a ¹H-NMR (CDCl₃) δ 0.86(1H, m), 1.08–1.60 (15H, m), 1.95(1H, m), 2.15 (1H, brs), 2.33 (2H, t,J=7.5 Hz), 3.26 (1H, m), 3.49 (1H, m), 6.15 (1H, brt, J=5.1 Hz), 6.33(2H, t, J=2.4 Hz), 7.16 (2H, t, J=2.4 Hz), 7.33 and 7.57 (each 1H, eachd, each J=3.9 Hz); IR (CHCl₃) 3514, 3446, 2677, 1709, 1660, 1533, 1508,1456, 1385, 1275, 1192, 1167, 1057, 1034 cm⁻¹; [α]_(D) ²⁴ − 7.6 ± 0.5°(c=1.006 MeOH) Anal. (C₂₃H₃₀N₂O₅S₂·0.3H₂O) Calcd.(%): C, 57.07; H, 6.37;N, 5.79; S, 13.25 Found (%): C, 57.16; H, 6.27; N, 5.81; S, 13.19VII-6A-47a ¹H-NMR (CDCl₃) δ 0.87 (1H, m), 1.10–1.63 (15H, m), 1.95 (1H,m), 2.16 (1H, brs), 2.33 (2H, t, J=7.5 Hz), 3.27 (1H, m), 3.49 (1H, m),6.23 (1H, brt, J=5.6 Hz), 7.11 (1H, dd, J=3.9 and 5.1 Hz), 7.38 and 7.63(each 1H, each d, each J=3.9 Hz), 7.70 (1H, dd, J=1.5 and 5.1 Hz), 7.75(1H, dd, J=1.5 and 3.9 Hz); IR (CHCl₃) 3514, 3446, 1709, 1657, 1533,1506, 1402, 1336, 1275, 1153, 1097, 1024 cm⁻¹; [α]_(D) ²⁴ − 8.1 ± 0.5°(c=1.008, MeOH) Anal. (C₂₃H₂₉NO₅S₃·0.3H₂O) Calcd.(%): C, 55.13; H, 5.95;N, 2.80; S, 19.20 Found (%): C, 55.15; H, 5.94; N, 3.06; S, 19.14VII-6A-88a ¹H-NMR (CDCl₃) δ 0.86 (1H, m), 1.09–1.61 (15H, m), 1.94 (1H,m), 2.17 (1H, brs), 2.32 (2H, t, J=7.5 Hz), 3.21 (1H, m), 3.52 (1H, m),4.15 (2H, s), 5.89 (1H, brt, J=5.4 Hz), 6.78 (1H, d, J=3.6 Hz), 6.96(1H, dd, J=1.8 and 5.1 Hz), 7.05 (1H, m), 7.28 (1H, dd, J=3.0 and 5.1Hz), 7.34 (1H, d, J=3.6 Hz); IR (CHCl₃) 3517, 3450, 1709, 1645, 1547,1514, 1462 cm⁻¹; [α]_(D) ²⁴ − 9.4 ± 0.5° (c=1.012, MeOH) Anal.(C₂₄H₃₁NO₃S₂) Calcd.(%): C, 64.68; H, 7.01; N, 3.14; S, 14.39 Found (%):C, 64.51; H, 6.90; N, 3.17; S, 14.53

The structure and physical property of the compound prepared as theexample of reference are shown below. A compound with a beginning number“I-” means a compound of the formula:

A compound with a beginning number “II-” means a compound of theformula:

A compound with a beginning number “III-” means a compound of theformula:

A compound with a beginning number “IV-” means a compound of theformula:

A compound with a beginning number “V-” means a compound of the formula:

A compound with a beginning number “VI-” means a compound of theformula:

Furthermore, a number following the number (I, II, III, IV, V, and VI)represents a structure of the group of the formula: —X¹—X²—X³ and eachnumber is the same meaning as that used in the list of the structure ofthe formula: —X¹—X²—X³.Compound Number I-1

mp.113–114° C.; ¹H-NMR(CDCl₃) δ: 1.09(1H, m), 1.17–1.32(2H, m),1.34–1.52(2H, m), 1.56–1.75(4H, m), 2.00–2.18(5H, m), 2.35 (2H, t, J=7.2Hz), 2.52(1H, m), 3.80(1H, m), 5.31–5.43(2H, m), 6.22(1H, d, J=6.0 Hz),6.35 and 7.17(each 2H, each t, each J=2.1 Hz), 7.37 and 7.56(each 1H,each d, each J=3.9 Hz). IR(Nujol): 3369, 3143, 3124, 3068, 2678, 1710,1626, 1593, 1374, 1200, 1171 cm⁻¹. [α]_(D) ^(26.5)+75.5±1.2°(c=1.004,MeOH) Anal. (C₂₃H₂₈N₂O₅S₂) Calcd.(%): C, 57.96.; H, 5.92; N, 5.88; S,13.45. Found(%): C, 57.99; H, 5.88; N, 5.66; S, 13.50.

Compound Number I-3

¹H-NMR (CDCl₃-CD₃OD) δ: 1.23(1H, m), 1.28–1.32(2H, m), 1.44–1.53(2H, m),1.57–1.74(4H, m), 2.03–2.14(5H, m), 2.32(2H, t, J=7.2 Hz), 2.56(1H, m),3.82(1H, m), 5.33–5.47(2H, m), 6.80(1H, m), 7.09–7.12(2H, m), 7.22(1H,t, J=8.1 Hz), 7.63 and 7.86(each 1H, each d, each J=8.1 Hz). IR(CHCl₃):3593 3442, 3111, 1710, 1644, 1519, 1449 cm⁻¹. [α]_(D)²⁵+77.6±1.20°(c=1.010, MeOH) Anal. (C₂₅H₂₉NO₄S.0.2H₂O) Calcd.(%): C,67.76; H, 6.69; N, 3.16; S, 7.23. Found(%): C, 67.64; H, 6.77; N, 3.17;S, 7.18.

Compound Number I-4

¹H-NMR(CDCl₃) δ: 1.06(1H, m), 1.17–1.32(2H, m), 1.40–1.50(2H, m),1.56–1.80 (4H, m), 2.00–2.22(5H, m), 2.33(2H, t, J=7.2 Hz), 2.53(1H, m),3.84 (3H, s), 3.85(1H, m), 5.29–5.42(2H, m), 6.18(1H, d, J=6.9 Hz),6.93, 7.10, 7.44 and 7.59 (each 2H, each d-like). IR(CHCl₃): 3516, 3448,1708, 1650, 1594, 1514, 1494, 1483, 1288, 1248, 1032 cm⁻¹. [α]_(D)²⁶+82.8±1.2°(c=1.000, MeOH) Anal. (C₂₈H₃₃NO₄S.0.2H₂O) Calcd.(%): C,69.59; H, 6.97; N, 2.90; S, 6.64. Found(%): C, 69.69; H, 6.93; N, 3.20;S, 6.57.

Compound Number I-5

¹H-NMR(CDCl₃) δ: 1.06(1H, m), 1.16–1.32(2H, m), 1.36–1.50(2H, m),1.54–1.80 (4H, m), 2.00–2.22(5H, m), 2.34(2H, t, J=7.2 Hz), 2.53(1H, m),3.82 (1H, m), 3.83(3H, s), 5.29–5.42(2H, m), 6.14(1H, d, J=7.2 Hz), 6.92(2H, d-like), 7.20–7.30(2H, m), 7.41–7.51(4H, m). IR(CHCl₃): 3509, 3444,2666, 1708, 1654, 1592, 1570, 1510, 1494, 1468, 1288, 1247, 1082 cm⁻¹.[α]_(D) ²⁶+58.4±1.4°(c=0.704, MeOH) Anal. (C₂₈H₃₃NO₄S.0.2H₂O) Calcd.(%):C, 69.59; H, 6.97; N, 2.90; S, 6.64. Found(%): C, 69.55; H, 6.93; N,3.03; S, 6.57.

Compound Number I-6

¹H-NMR(CDCl₃) δ: 1.11(1H, m), 1.20–1.34(2H, m), 1.42–1.52(2H, m),1.56–1.78(4H, m), 2.00–2.23(5H, m), 2.35(2H, t, J=7.2 Hz), 2.57(1H, m),3.89 (1H, m), 5.31–5.45(2H, m), 6.30(1H, d, J=7.2 Hz), 6.37 and7.12(each 2H, each 2H, each J=2.1 Hz), 7.42 and 7.83(each 2H, eachd-like). IR(CHCl₃): 3518, 3448, 2662, 1708, 1653, 1609, 1499, 1334 cm⁻¹.[α]_(D) ²³+94.9±1.3°(c=1.005, MeOH) Anal. (C₂₅H₃₀N₂O₃.0.1H₂O) Calcd.(%):C, 73.54; H, 7.45; N, 6.86. Found(%): C, 73.43; H, 7.46; N, 7.01.

Compound Number I-7

¹H-NMR(CDCl₃) δ: 1.12–1.76(9H, m), 1.96–2.24(5H, m), 2.33(2H, t, J=7.2Hz), 2.53(1H, m), 3.86(1H, m), 5.30–5.47(2H, m), 6.60(1H, d, J=6.9 Hz),7.05–7.23(5H, m), 7.55(1H, brs), 7.67 and 7.74(each 2H, each d, eachJ=8.7 Hz). IR(CHCl₃): 3516, 3439, 3368, 1708, 1653, 1600, 1519, 1496,1487, 1401, 1347, 1165 cm⁻¹. [α]_(D) ²⁵+69.9±1.1°(c=1.019, MeOH) Anal.(C₂₇H₃₄N₂O₅S.0.1H₂O) Calcd.(%): C, 64.80; H, 6.89; N, 5.60; S, 6.41.Found(%): C, 64.73; H, 6.56; N, 5.74; S, 6.41.

Compound Number I-8

¹H-NMR(CDCl₃) δ: 1.19–1.27(3H, m), 1.35–1.43(2H, m), 1.55–1.80(4H, m),1.90–2.08(3H, m), 2.11–2.21(2H, m), 2.34(2H, t, J=7.2 Hz), 2.53(1H, m),3.74 (1H, m), 5.29–5.48(2H, m), 6.44(1H, d, J=6.9 Hz), 7.15(1H, d, J=1.5Hz), 7.46(2H, t, J=7.8 Hz), 7.57(1H, m), 7.60(1H, d, J=1.5 Hz),7.76–7.78 (2H, m), 7.89(1H, s). IR(CHCl₃): 3440, 3360, 3107, 1708, 1637,1518, 1448, 1329, 1163 cm⁻¹. [α]_(D) ²⁰+55.5±1.0°(c=1.003, MeOH) Anal.(C₂₅H₃₀N₂O₅S₂.0.2H₂O) Calcd.(%): C, 59.31; H, 6.05; N, 5.53; S, 12.67.Found(%): C, 59.19; H, 6.12; N, 5.66; S, 12.50.

Compound Number I-9

mp.193–194° C.; ¹H-NMR (d₆-DMSO) δ: 1.18–1.59 (9H, m), 1.93 (1H, d,J=2.4 Hz), 1.99–2.07(4H, m), 2.21(2H, t, J=7.2 Hz), 2.36(1H, m),5.30–5.40(2H, m), 7.25(1H, d, J=1.5 Hz), 7.54–7.63(3H, m), 7.69(1H, d,J=1.5 Hz), 7.99–8.02 (3H, m), 11.6(1H, s), 12.00(1H, brs). IR(Nujol):3367, 3221, 3186, 3091, 3055, 2654, 1711, 1631, 1566, 1541, 1321 cm⁻¹.[α]_(D) ²¹+74.6±1.1°(c=1.006, MeOH) Anal. (C₂₆H₃₀N₂O₄S) Calcd.(%): C,66.93; H, 6.48; N, 6.00; S, 6.87. Found(%): C, 66.76; H, 6.44; N, 5.88;S, 6.76.

Compound Number I-10

¹H-NMR(CDCl₃) δ: 1.08(1H, m), 1.18–1.34(2H, m), 1.40–1.50(2H, m),1.56–1.77(4H, m), 2.00–2.20(5H, m), 2.35(2H, t, J=7.2 Hz), 2.55(1H, m),3.86 (1H, m), 5.31–5.54(2H, m), 6.26(1H, d, J=7.8 Hz), 6.31 and7.14(each 2H, each t, each J=2.1 Hz), 7.84 and 7.88(each 2H, each d,each J=8.4 Hz). IR(CHCl₃): 3515, 3441, 3144, 2669, 1708, 1662, 1515,1486, 1455, 1376 cm⁻¹. [α]_(D) ²²+77.4±1.2°(c=1.004, MeOH) Anal.(C₂₅H₃₀N₂O₅S.0.2H₂O) Calcd.(%): C, 63.32; H, 6.46; N, 6.91; S, 6.76.Found(%): C, 63.23; H, 6.49; N, 5.88; S, 6.67.

Compound Number I-11

¹H-NMR(CDCl₃) δ: 1.06(1H, m), 1.18–1.29(2H, m), 1.42–1.46(2H, m),1.56–1.79 (4H, m), 2.03–2.20(5H, m), 2.34(2H, t, J=7.2 Hz), 2.52(1H, m),3.82(1H, m), 4.12(2H, s), 5.29–5.43(2H, m), 6.04(1H, d, J=7.5 Hz),7.09(1H, d, J=1.5 Hz), 7.22–7.34(5H, m), 7.67(1H, d, J=1.5 Hz). IR(CHCl₃): 3517, 3446, 2669, 1708, 1647, 1549, 1508, 1454 cm⁻¹. [α]_(D)^(21.5)+68.8±1.1°(c=1.016, MeOH) Anal. (C₂₆H₃₁NO₃S.0.1H₂O) Calcd.(%): C,71.07; H, 7.16; N, 3.19; S, 7.30. Found(%): C, 71.05; H, 7.11; N, 3.38;S, 7.33.

Compound Number I-12

¹H-NMR(CDCl₃) δ: 1.09(1H, m), 1.10–1.30(2H, m), 1.40–1.46(2H, m),1.56–1.77 (4H, m), 2.00–2.22(5H, m), 2.33(2H, t, J=7.2 Hz), 2.52(1H, m),3.83(1H, m), 5.28–5.42 (2H, m), 6.26(1H, d, J=6.9 Hz), 7.15 and7.63(each 2H, each d, each J=8.7 Hz), 7.53(1H, m), 7.78–7.82(2H, m).IR(CHCl₃): 3515, 3446, 3371, 3138, 1708, 1648, 1610, 1496, 1163 cm⁻¹.[α]_(D) ^(22.5)+66.5±1.1°(c=1.004, MeOH) Anal. (C₂₇H₃₄N₂O₅S.0.4H₂O)Calcd.(%): C, 64.11; H, 6.93; N, 5.54; S, 6.34. Found(%): C, 64.05; H,6.63; N, 5.56; S, 6.12.

Compound Number I-13

¹H-NMR(CDCl₃) δ: 1.19–1.31(3H, m), 1.36–1.44(2H, m), 1.55–1.78(4H, m),1.85–2.02(2H, m), 2.05(1H, m), 2.13–2.47(4H, m), 2.57(1H, m), 3.71(1H,m), 5.31–5.54(2H, m), 6.53(1H, d, J=6.9 Hz), 7.14–7.32(5H, m), 7.47(1H,br), 8.05 and 8.13 (each 1H, each d, each J=1.5 Hz). IR(CHCl₃): 3509,3360, 3262, 1709, 1649, 1542, 1496, 1349, 1160 cm⁻¹. [α]_(D)²³+59.1±1.1°(c=1.001, MeOH) Anal. (C₂₅H₃₀N₂O₅S₂.0.2H₂O) Calcd.(%): C,59.31; H, 6.05; N, 5.53; S, 12.67. Found(%): C, 59.17; H, 6.01; N, 5.49;S, 12.37.

Compound Number I-14

¹H-NMR(CDCl₃) δ: 1.18–1.32(3H, m), 1.38–1.47(2H, m), 1.55–1.78(4H, m),1.90–2.08(3H, m), 2.15–2.31(2H, m), 2.32–2.49(2H, m), 2.59(1H, m), 3.74(1H, m), 5.33–5.53(2H, m), 6.35 and 7.17(each 2H, each t, each J=2.4Hz), 6.47(1H, d, J=6.3 Hz), 8.21 and 8.22(each 1H, each d, each J=1.5Hz). IR(CHCl₃): 3506, 3412, 3144, 3107, 1727, 1709, 1656, 1540, 1504,1456, 1382, 1166 cm⁻¹. [α]_(D) ²³+63.8±1.0°(c=1.005, MeOH) Anal.(C₂₃H₂₈N₂O₅S₂.0.2H₂O) Calcd.(%): C, 57.53; H, 5.96; N, 5.83; S, 13.35.Found(%): C, 57.44; H, 5.96; N, 6.00; S, 13.35.

Compound Number I-15

mp.128–130° C.; ¹H-NMR(CDCl₃) δ: 1.16–1.34(3H, m), 1.40–1.81(6H, m),2.37 (2H, t, J=7.2 Hz), 2.57(1H, m), 3.89(1H, m), 5.35–5.51(2H, m), 6.37and 7.20 (each 2H, each d, each J=2.4 Hz), 7.23(1H, d, J=8.7 Hz). IR(Nujol): 3371, 3097, 2662, 1716, 1703, 1671, 1652, 1530, 1367, 1361,1187, 1162 cm⁻¹. [α]_(D) ²⁵+47.5±0.9°(c=1.003, MeOH) Anal.(C₂₃H₂₈N₂O₅S₂) Calcd.(%): C, 57.96; H, 5.92; N, 5.88; S, 13.45.Found(%): C, 58.05; H, 5.91; N, 5.83; S, 13.38.

Compound Number I-16

¹H-NMR(CDCl₃) δ: 1.09(1H, m), 1.20–1.32(2H, m), 1.42–1.47(2H, m),1.58–1.75(4H, m), 2.01(3H, d, J=2 Hz), 2.00–2.16(5H, m), 2.35(2H, t,J=7.2 Hz), 2.55(1H, m), 3.86(1H, m), 5.31–5.44(2H, m), 6.14(1H, dd,J=1.5 and 3.0 Hz), 6.29(1H, d, J=7.5 Hz), 6.86(1H, m), 7.04(1H, t, J=3.0Hz), 7.84 (4H, s). IR(CHCl₃): 3517, 3441, 2667, 1708, 1661, 1515, 1485,1375, 1260, 1178 cm⁻¹. [α]_(D) ²⁵+73.8±1.1°(c=1.001, MeOH) Anal.(C₂₆H₃₂N₂O₅S.0.1H₂O) Calcd.(%): C, 64.20; H, 6.67; N, 5.76; S, 6.59.Found(%): C, 64.14; H, 6.65; N, 5.85; S, 6.86.

Compound Number I-17

¹H-NMR(CDCl₃) δ: 1.20–1.31(3H, m), 1.40–1.47(2H, m), 1.57–1.80(4H, m),2.00–2.30(5H, m), 2.37(2H, t, J=6.9 Hz), 2.60(1H, m), 3.84(1H, m),5.32–5.50(2H, m), 6.32(2H, t, J=2.4 Hz), 6.63(1H, d, J=6.6 Hz), 7.16(2H,t, J=2.4 Hz), 7.55(1H, t, J=8.0 Hz), 7.89(1H, m), 8.06(1H, d, J=7.8 Hz),8.30(1H, t, J=1.7 Hz). IR(CHCl₃): 3394, 3145, 1726, 1709, 1659, 1374cm⁻¹. [α]_(D) ²⁵+60.3±1.0°(c=1.000, MeOH) Anal. (C₂₅H₃₀N₂O₅S.0.2H₂O)Calcd.(%): C, 63.32; H, 6.46; N, 5.91; S, 6.76. Found(%): C, 63.39; H,6.50; N, 6.16; S, 6.80.

Compound Number I-18

¹H-NMR(CDCl₃) δ: 1.10(1H, m), 1.20–1.32(2H, m), 1.45(2H, t, J=6.9 Hz),1.58–1.74(4H, m), 2.04–2.16(5H, m), 2.28(3H, s), 2.35(2H, t, J=6.9 Hz),2.55 (1H, m), 3.87(1H, m), 5.31–5.44(2H, m), 5.96(1H, m), 6.18(1H, t,J=3.3 Hz), 6.32 (1H, d, J=7.5 Hz), 7.25(1H, dd, J=1.8 and 3.3 Hz), 7.78and 7.85(each 2H, each d, each J=8.7 Hz). IR(CHCl₃): 3514, 3441, 1708,1661, 1515, 1487, 1368, 1164 cm⁻¹. [α]_(D) ²⁵+74.0±1.1°(c=1.004, MeOH)Anal. (C₂₆H₃₂N₂O₅S.0.2H₂O) Calcd.(%): C, 63.96; H, 6.69; N, 5.74; S,6.57. Found(%): C, 63.97; H, 6.69; N, 5.98; S, 6.54.

Compound Number I-19

¹H-NMR(CDCl₃) δ: 1.07(1H, m), 1.18–1.31(2H, m), 1.41–1.49(2H, m),1.56–1.76(4H, m), 2.00–2.21(5H, m), 2.34(2H, t, J=7.2 Hz), 2.55(1H, m),3.86 (1H, m), 5.09(2H, s), 5.29–5.43(2H, m), 6.19(2H, t, J=2.1 Hz),6.25(1H, d, J=7.5 Hz), 6.67(2H, t, J=2.1 Hz), 7.13 and 7.70(each 2H,each d, each J=8.4 Hz). IR(CHCl₃): 3517, 3446, 3103, 2667, 1708, 1653,1523, 1497 cm⁻¹. [α]_(D) ²⁵+57.7±1.0°(c=1.010, MeOH) Anal. (C₂₆H₃₂N₂O₃)Calcd.(%): C, 73.63; H, 7.70; N, 6.60. Found(%): C, 73.72; H, 7.77; N,6.76.

Compound Number I-20

¹H-NMR(CDCl₃) δ: 1.05(1H, m), 1.15–1.30(2H, m), 1.36–1.45(2H, m),1.55–1.72 (4H, m), 2.00–2.14(5H, m), 2.32(2H, t, J=7.2 Hz), 2.51(1H, m),3.82 (1H, m), 5.28–5.42(2H, m), 6.22(2H, d, J=7.5 Hz), 6.68(1H, d, J=3.6Hz), 7.22–7.34(2H, m), 7.52–7.55(2H, m), 7.76 and 7.88(each 2H, each d,each J=8.7 Hz), 7.97(1H, d, J=8.1 Hz). IR(CHCl₃): 3510, 3480, 3440,3145, 3117, 1708, 1661, 1516, 1485, 1445, 1377, 1130 cm⁻¹. [α]_(D)²⁵+65.9±1.1°(c=1.010, MeOH) Anal. (C₂₉H₃₂N₂O₅S.0.3H₂O) Calcd.(%): C,66.21; H, 6.25; N, 5.33; S, 6.10. Found(%): C, 66.34; H, 6.30; N, 5.63;S, 5.84.

Compound Number I-21

¹H-NMR(CDCl₃) δ: 1.13(1H, m), 1.20–1.31(2H, m), 1.44(2H, t, J=6.8 Hz),1.59–1.72(4H, m), 2.03–2.20(5H, m), 2.32(2H, t, J=7.2 Hz), 2.54(1H, m),3.83 (1H, m), 4.62(2H, s), 5.31–5.45(2H, m), 6.25–6.26(2H, m), 6.57(1H,d, J=7.2 Hz), 7.25(1H, m), 7.81(4H, s). IR(CHCl₃): 3581, 3518, 3440,3149, 1708, 1660, 1517, 1486, 1371, 1150 cm⁻¹. [α]_(D)²⁷+72.2±1.1°(c=1.007, MeOH) Anal. (C₂₆H₃₂N₂O₆S) Calcd.(%): C, 62.38; H,6.44; N, 5.60; S, 6.40. Found(%): C, 62.17; H, 6.52; N, 5.71; S, 6.40.

Compound Number I-22

¹H-NMR(d₆-DMSO) δ: 1.18–1.33(3H, m), 1.43–1.60(6H, m), 1.92–2.30(5H, m),2.20(2H, t, J=7.5 Hz), 2.38(1H, m), 3.67(1H, m), 5.30–5.36(2H, m), 6.85(1H, d, J=4.8 Hz), 7.27(1H, d, J=4.8 Hz), 7.86 and 7.94(each 2H, each d,each J=8.7 Hz), 8.37(1H, d, J=6.9 Hz). IR(KBr): 3360, 3151, 3103, 1707,1635, 1569, 1530, 1328, 1284, 1140 cm⁻¹. [α]_(D) ²⁷+67.4±1.1°(c=1.007,DMSO) Anal. (C₂₄H₂₉N₃O₅S₂.0.3H₂O) Calcd.(%): C, 56.62; H, 5.86; N, 8.24;S, 12.60. Found(%): C, 56.74; H, 5.96; N, 8.30; S, 12.31.

Compound Number I-23

mp.231–232° C.; ¹H-NMR(d₆-DMSO) δ: 1.19–1.61(9H, m), 1.95–2.08(5H, m),2.21(2H, t, J=7.2 Hz), 2.40(1H, m), 3.71(1H, m), 5.34–5.37(2H, m), 7.31and 7.59(each 1H, each d, each J=3.6 Hz), 7.98 and 8.16(each 2H, each d,each J=8.7 Hz), 8.41(1H, d, J=7.2 Hz). IR(KBr): 3336, 3185, 2541, 1675,1631, 1548, 1324, 1295, 1163 cm⁻¹. [α]_(D) ²⁷+84.5±1.3°(c=1.000, DMSO)Anal. (C₂₄H₂₉N₃O₄S) Calcd.(%):.C, 64.22; H, 6.25; N, 8.99; S, 6.86.Found(%): C, 64.13; H, 6.10; N, 8.92; S, 7.08.

Compound Number I-24

¹H-NMR(CDCl₃) δ: 1.14(1H, m), 1.22–1.35(2H, m), 1.44–1.53(2H, m),1.58–1.78 (4H, m), 2.02–2.28(5H, m), 2.36(2H, t, J=7.2 Hz), 2.58(1H, m),3.87(1H, m), 5.15–5.48(2H, m), 6.29 and 7.18(each 2H, each t, J=2.4 Hz),6.38(1H, d, J=7.2 Hz), 7.77(1H, dd, J=1.8 and 8.7 Hz), 7.82(1H, s),7.91(1H, d, J=8.7 Hz), 8.34(1H, d, J=1.8 Hz). IR(CHCl₃): 3512, 3441,3423, 3144, 2670, 1708, 1530, 1501, 1374, 1164 cm⁻¹. [α]_(D)²⁶+96.1±1.4°(c=1.006, MeOH) Anal. (C₂₇H₃₀N₂O₅S₂.0.2H₂O) Calcd.(%): C,61.16; H, 5.78; N, 5.28; S, 12.09. Found(%): C, 61.17; H, 5.74; N, 5.35;S, 12.12.

Compound Number I-25

¹H-NMR(CDCl₃) δ: 1.06(1H, m), 1.17–1.31(2H, m), 1.39–1.48(2H, m),1.56–1.77(4H, m), 1.99–2.20(5H, m), 2.34(2H, t, J=7.2 Hz), 2.53(1H, m),3.84 (1H, m), 5.29–5.42(2H, m), 6.20(1H, d, J=7.2 Hz), 7.10–7.17(3H, m),7.32 (1H, dd, J=1.2 and 3.6 Hz), 7.54(1H, dd, J=1.2 and 5.4 Hz),7.60–7.64 (2H, m). IR(CHCl₃): 3518, 3447, 2669, 1708, 1651, 1596, 1515,1483 cm⁻¹. [α]_(D) ²⁶+84.7±1.2°(c=1.003, MeOH) Anal.(C₂₅H₂₉NO₃S₂.0.1H₂O) Calcd.(%): C, 65.64; H, 6.43; N, 3.06; S, 14.02.Found(%): C, 65.58; H, 6.41; N, 3.10; S, 13.82.

Compound Number I-26

¹H-NMR(CDCl₃) δ: 1.13(1H, m), 1.20–1.33(2H, m), 1.41–1.50(2H, m),1.56–1.77(4H, m), 2.00–2.21(5H, m), 2.37(2H, t, J=7.2 Hz), 2.55(1H, m),3.87(1H, m), 5.31–5.45(2H, m), 6.48(1H, d, J=7.2 Hz), 7.10(1H, dd, J=3.9and 5.1 Hz), 7.68(1H, dd, J=1.2 and 5.1 Hz), 7.69(1H, dd, J=1.2 and 3.9Hz), 7.84–7.88 and 7.95–7.99(each 2H, each m). IR(CHCl₃): 3518, 3441,3382, 1708, 1659, 1515, 1329, 1158 cm⁻¹. [α]_(D) ²⁶+75.7±1.2°(c=1.000,MeOH) Anal. (C₂₅H₂₉NO₅S₂) Calcd.(%): C, 61.58; H, 5.99; N, 2.87; S,13.15. Found(%): C, 61.36; H, 6.05; N, 2.91; S, 13.13.

Compound Number I-27

mp.213–215° C.; ¹H-NMR(d₆-DMSO) δ: 1.18–1.61(9H, m), 1.95–2.10 (5H, m),2.21(2H, t, J=7.5 Hz), 2.40(1H, m), 3.71(1H, m), 5.33–5.38(2H, m),7.19(1H, m), 7.87(1H, m), 7.96 and 8.10(each 2H, each d, each J=8.2 Hz),8.21(1H, d, J=8.6 Hz), 8.40(1H, m), 10.92(1H, s), 12.05(1H, brs). IR(Nujol): 3337, 3249, 3205, 3132, 2524, 1678, 1632, 1545, 1433, 1305cm⁻¹. [α]_(D) ²³+85.2±2.5°(c=0.505, MeOH) Anal. (C₂₇H₃₁N₃O₄.0.3H₂O)Calcd.(%): C, 69.72; H, 6.80; N, 9.03. Found(%): C, 69.76; H, 6.75; N,8.76.

Compound Number I-28

¹H-NMR(CDCl₃) δ: 1.07(1H, m), 1.18–1.32(2H, m), 1.40–1.50(2H, m),1.56–1.78(4H, m), 2.00–2.21(5H, m), 2.34(2H, t, J=7.2 Hz), 2.54(1H, m),3.85 (1H, m), 5.29–5.42(2H, m), 6.17(1H, d, J=6.9 Hz), 7.07(1H, dd,J=1.2 and 5.1 Hz), 7.15(2H, d J=8.7 Hz), 7.43(1H, dd, J=3.0 and 5.1 Hz),7.51(1H, dd, J=1.2 and 3.0 Hz), 7.62(2H, d, J=8.7 Hz). IR(CHCl₃): 3510,3447, 3110, 2666, 1708, 1651, 1596, 1515, 1482 cm⁻¹. [α]_(D)²⁷+85.9±1.3°(c=1.007, MeOH) Anal. (C₂₅H₂₉NO₃S₂) Calcd.(%): C, 65.90; H,6.42; N, 3.07; S, 14.07. Found(%): C, 65.60; H, 6.36; N, 3.36; S, 13.86.

Compound Number I-29

mp.123–125° C.; ¹H-NMR (CDCl₃) δ: 1.12(1H, m), 1.18–1.34(2H, m),1.42–1.50(2H, m), 1.56–1.78(4H, m), 2.02–2.21(5H, m), 2.35(2H, t, J=7.2Hz), 2.55(1H, m), 3.88(1H, m), 5.31–5.45(2H, m), 6.42(1H, d, J=6.0 Hz),7.31 (1H, d, J=5.1 Hz), 7.40(1H, dd, J=3.0 and 5.1 Hz), 7.87 and7.96(each 2H, each d, each J=8.7 Hz), 8.11(1H, d, J=3.0 Hz). IR(Nujol):3286, 3108, 2671, 1701, 1641, 1546, 1327, 1156 cm⁻¹. [α]_(D)²⁷+75.3±1.2°(c=1.004, MeOH) Anal. (C₂₅H₂₉NO₅S₂) Calcd.(%): C, 61.58; H,5.99; N, 2.87; S, 13.15. Found(%): C, 61.39; H, 5.94; N, 3.02; S, 12.99.

Compound Number I-30

¹H-NMR(CDCl₃) δ: 1.12(1H, m), 1.23–1.34(2H, m), 1.43–1.52(2H, m),1.58–1.79(4H, m), 2.02–2.24(5H, m), 2.36(2H, t, J=7.2 Hz), 2.53(1H, m),3.87 (1H, m), 5.32–5.45(2H, m), 6.11(1H, d, J=3.6 Hz), 6.28(1H, d, J=7.5Hz), 6.35 and 7.09(each 2H, each t, each J=2.1 Hz), 7.16(1H, d, J=3.6Hz). IR (CHCl₃): 3512, 3438, 3142, 1741, 1709, 1653, 1623, 1564, 1508cm⁻¹. [α]_(D) ²⁵+102.4±1.4°(c=1.006, MeOH) Anal. (C₂₃H₂₈N₂O₄.0.2H₂O)Calcd.(%): C, 69.05; H, 7.15; N, 7.00. Found(%): C, 69.12; H, 7.10; N,6.95.

Compound Number I-31

¹H-NMR(CDCl₃) δ: 1.04(1H, m), 1.08–1.28(2H, m), 1.41–1.46(2H, m),1.55–1.78(4H, m), 1.99–2.16(5H, m), 2.34(2H, t, J=7.2 Hz), 2.51(1H, m),3.81(1H, m), 4.13(2H, s), 5.29–5.42(2H, m), 5.96(1H, d, J=8.1 Hz),6.77(1H, ddd, J=0.9, 0.9 and 3.9 Hz), 7.20–7.35(5H, m), 7.37(1H, d,J=3.9 Hz). IR (CHCl₃): 3511, 3445, 2670, 1708, 1642, 1544, 1507, 1455cm⁻¹. [α]_(D) ²⁶+67.1±1.1°(c=1.015, MeOH) Anal. (C₂₆H₃₁NO₃S) Calcd.(%):C, 71.36; H, 7.14; N, 3.20; S, 7.33. Found(%): C, 71.19; H, 7.16; N,3.34; S, 7.26.

Compound Number I-32

¹H-NMR(CDCl₃) δ: 1.22–1.85(9H, m), 1.95–2.53(7H, m), 2.66(1H, m),3.84(1H, m), 5.37–5.60(2H, m), 6.79(1H, d, J=6.0 Hz), 7.01–7.17(5H, m),7.83 (1H, dd J=1.5 and 8.7 Hz), 7.53(1H, d, J=8.7 Hz), 7.89(1H, s), 8.35(1H, s), 8.83(1H, d, J=1.5 Hz). IR(CHCl₃): 3509, 3437, 3364, 3209, 1710,1634, 1495, 1344, 1158 cm⁻¹. [α]_(D) ²⁶+36.6±0.8°(c=1.005, MeOH) Anal.(C₂₉H₃₂N₂O₅S₂.0.2H₂O) Calcd.(%): C, 62.61; H, 5.87; N, 5.04; S, 11.53.Found(%): C, 62.53; H, 5.87; N, 5.21; S, 11.42.

Compound Number I-33

¹H-NMR(CDCl₃) δ: 1.13(1H, m), 1.20–1.37(2H, m), 1.46–1.56(2H, m),1.60–1.80 (4H, m), 2.02–2.28(5H, m), 2.38(2H, t, J=7.2 Hz), 2.64(1H, m),3.94 (1H, m), 5.35–5.50(2H, m), 6.21(1H, d, J=7.2 Hz), 6.28 and7.21(each 2H, each t, each J=2.4 Hz), 7.81(1H, dd, J=1.8 and 8.7 Hz),7.91(1H, d, J=8.7 Hz), 7.99(1H, s), 8.97(1H, d, J=1.8 Hz). IR(CHCl₃):3513, 3438, 3144, 3096, 1708, 1656, 1518, 1374 cm⁻¹. [α]_(D)²⁶+40.1±0.8°(c=1.010, MeOH) Anal. (C₂₇H₃₀N₂O₅S₂.0.2H₂O) Calcd.(%): C,61.16; H, 5.78; N, 5.28; S, 12.09. Found(%): C, 61.16; H, 5.76; N, 5.43;S, 12.05.

Compound Number I-34

¹H-NMR(CDCl₃) δ: 1.18–1.35(3H, m), 1.40–1.48(2H, m), 1.57–1.79(4H, m),1.99–2.21(5H, m), 2.37(2H, t, J=7.2 Hz), 2.50(1H, m), 3.80(1H, m),5.32–5.47(2H, m), 6.38(2H, t, J=2.4 Hz), 6.54(1H, d, J=7.5 Hz), 7.12 and7.13(each 1H, each d, each J=3.6 Hz), 7.20(2H, t, J=2.4 Hz). IR(CHCl₃):3512, 3433, 3144, 2686, 1708, 1669, 1591, 1528, 1475, 1457, 1394 cm⁻¹.[α]_(D) ²⁶+74.3±1.1°(c=1.007, MeOH) Anal. (C₂₃H₂₈N₂O₅S) Calcd.(%): C,59.98; H, 6.13; N, 6.08; S, 6.96. Found(%): C, 59.71; H, 6.22; N, 6.10;S, 7.02.

Compound Number I-35

mp.102–103° C.; ¹H-NMR(CDCl₃) δ: 1.05(1H, m), 1.18–1.30(2H, m),1.38–1.48(2H, m), 1.55–1.78(4H, m), 1.99–2.19(5H, m), 2.35(2H, t, J=7.2Hz), 2.52(1H, m), 3.81(1H, m), 5.20(2H, d, J=0.9 Hz), 5.30–5.42(2H, m),5.99 (1H, d, J=7.2 Hz), 6.20 and 6.71 (each 2H, each t, each J=2.1 Hz),6.86(1H, td, J=0.9 and 3.9 Hz), 7.37(1H, d, J=3.9 Hz). IR(Nujol): 3393,3093, 6064, 2669, 1704, 1616, 1523, 1522 cm⁻¹. [α]_(D)²⁶+71.1±1.1°(c=1.005, MeOH) Anal. (C₂₄H₃₀N₂O₃S) Calcd.(%): C, 67.58; H,7.09; N, 6.57; S, 7.52. Found(%): C, 67.45; H, 7.09; N, 6.58; S, 7.67.

Compound Number I-36

¹H-NMR(CDCl₃) δ: 1.07(1H, m), 1.18–1.31(2H, m), 1.40–1.48(2H, m),1.56–1.78(4H, m), 2.00–2.20(5H, m), 2.35(2H, t, J=7.2 Hz), 2.53(1H, m),3.82 (1H, m), 5.31–5.43(2H, m), 6.02(1H, d, J=7.2 Hz), 7.15 and 7.44(each 1H, each d, each J=3.9 Hz), 7.20–7.33(5H, m). IR(CHCl₃): 3511,3444, 3426, 3031, 2665, 1708, 1646, 1530, 1499, 1477, 1421, 1318 cm⁻¹.[α]_(D) ²⁶+74.8±1.1°(c=1.004, MeOH) Anal. (C₂₅H₂₉NO₃S₂) Calcd.(%): C,65.90; H, 6.42; N, 3.07; S, 14.07. Found(%): C, 65.61; H, 6.40; N, 3.19;S, 14.18.

Compound Number I-37

¹H-NMR(CDCl₃) δ: 1.09(1H, m), 1.17–1.31(2H, m), 1.38–1.47(2H, m),1.54–1.74(4H, m), 2.00–2.17(5H, m), 2.34(2H, t, J=7.2 Hz), 2.52(1H, m),3.80 (1H, m), 5.30–5.43(2H, m), 6.27(1H, d, J=7.2 Hz), 7.41(1H, d, J=4.2Hz), 7.51–7.64(4H, m), 7.98(2H, m). IR(CHCl₃): 3515, 3442, 3366, 1708,1656, 1530, 1504, 1327, 1156 cm⁻¹. [α]_(D) ²⁶+73.1±1.1°(c=1.004, MeOH)Anal. (C₂₅H₂₉NO₅S₂.0.2H₂O) Calcd.(%): C, 61.13; H, 6.03; N, 2.85; S,13.05. Found(%): C, 60.94; H, 6.02; N, 2.86; S, 3.12.

Compound Number I-38

mp.163–165° C. ¹H-NMR(CDCl₃) δ: 1.24–1.43(3H, m), 1.52–1.87 (8H, m),2.10(1H, d, J=3.0 Hz), 2.30–2.55(4H, m), 2.71(1H, m), 3.66(1H, m), 5.38and 5.63(each 1H, each m), 7.13(1H, d, J=1.5 Hz), 7.34(1H, d, J=5.4 Hz),7.49–7.60(3H, m), 7.86–7.89(2H, m), 8.49(1H, s), 8.69(1H, d, J=1.5 Hz).IR(KBr): 3367, 3261, 3090, 1726, 1645, 1618, 1589, 1577, 1535, 1513,1426, 1396, 1289, 1197 cm⁻¹. [α]_(D) ²³+84.5±1.2°(c=1.006, MeOH) Anal.(C₂₆H₃₀N₂O₄S) Calcd.(%): C, 66.93; H, 6.48; N, 6.00; S, 6.87. Found(%):C, 66.97; H, 6.36; N, 6.01; S, 6.89.

Compound Number I-39

¹H-NMR(CDCl₃) δ: 1.25–1.80(9H, m), 1.87–2.05(3H, m), 2.14–2.29(2H, m),2.37(2H, t, J=6.9 Hz), 2.57(1H, m), 3.73(1H, m), 5.35 and 5.49(each 1H,each m), 6.71(1H, d, J=6.6 Hz), 6.87(1H, d, J=1.5 Hz), 7.43–7.48(2H, m),7.56 (1H, m), 7.63(1H s), 7.64((1H, d, J=1.5 Hz), 7.73–7.76(2H, m). IR(CHCl₃): 3510, 3379, 3247, 3108, 1709, 1637, 1556, 1516, 1448, 1365,1319, 1161 cm⁻¹. [α]_(D) ²³+61.1±1.0°(c=1.004, MeOH) Anal.(C₂₅H₃₀N₂O₅S₂.0.2H₂O) Calcd.(%): C, 59.31; H, 6.05; N, 5.53; S, 12.67.Found(%): C, 59.38; H, 6.11; N, 5.75; S, 12.41.

Compound Number I-40

¹H-NMR(CDCl₃) δ: 1.11(1H, m), 1.24–1.31(2H, m), 1.44–1.52(2H, m),1.60–1.79 (4H, m), 2.00–2.21(5H, m), 2.37(2H, t, J=7.2 Hz), 2.56(1H, m),3.86 (1H, m), 5.32–5.46(2H, m), 6.11(1H, d, J=7.8 Hz), 7.25 and7.49(each 1H, each d, each J=4.2 Hz), 7.30–7.43(3H, m), 7.60–7.63(2H,m). IR(CHCl₃): 3510, 3445, 3428, 1739, 1708, 1643, 1540, 1510, 1491,1454 cm⁻¹. [α]_(D) ³⁵+88.0±1.3°(c=1.012, MeOH) Anal. (C₂₅H₂₉NO₃S.0.2H₂O)Calcd.(%): C, 70.29; H, 6.94; N, 3.28; S, 7.51. Found(%): C, 70.35; H,7.01; N, 3.59; S, 7.46.

Compound Number I-41

¹H-NMR(CDCl₃) δ: 1.13(1H, m), 1.22–1.32(2H, m), 1.46–1.51(2H, m),1.60–1.76(4H, m), 2.04–2.17(5H, m), 2.36(2H, t, J=7.2 Hz), 2.57(1H, m),3.86(1H, m), 5.32–5.46(2H, m), 6.30(1H, d, J=8.4 Hz), 7.48–7.65(5H, m),7.84–7.88(2H, m). IR(CHCl₃): 3511, 3443, 3425, 1708, 1643, 1529, 1506,1448 cm⁻¹. [α]_(D) ²⁵+92.4±1.3°(c=1.000, MeOH) Anal.(C₂₆H₂₉NO₄S₂.0.2H₂O) Calcd.(%): C, 68.61; H, 6.51; N, 3.08; S, 7.04.Found(%): C, 68.55; H, 6.52; N, 3.13; S, 7.03.

Compound Number I-42

¹H-NMR(CDCl₃) δ: 1.10(1H, m), 1.27–1.31(2H, m), 1.49(2H, brs), 1.59–1.80(4H, m), 2.00–2.20(5H, m), 2.36(2H, t, J=7.2 Hz), 2.55(1H, m), 3.85 (1H,m), 5.31–5.45(2H, m), 6.14(1H, d, J=7.2 Hz), 7.13(1H, d, J=3.9 Hz), 7.30(1H, dd, J=1.2 and 5.1 Hz), 7.36(1H, dd, J=3.0 and 5.1 Hz), 7.45–7.46(2H, m). IR(CHCl₃): 3511, 3445, 3428, 3109, 1708, 1642, 1523, 1499, 1456cm⁻¹. [α]_(D) ²⁵+82.9±1.20(c=1.006, MeOH) Anal. (C₂₃H₂₇NO₃S₂.0.1H₂O)Calcd.(%): C, 64.04; H, 6.36; N, 3.25; S, 14.86. Found(%): C, 63.99; H,6.52; N, 3.23; S, 14.85.

Compound Number I-43

¹H-NMR(CDCl₃) δ: 1.10(1H, m), 1.22–1.31(2H, m), 1.46–1.51(2H, m),1.60–1.80(4H, m), 2.03–2.22(5H, m), 2.37(2H, t, J=7.2 Hz), 2.55(1H, m),3.85 (1H, m), 5.32–5.45(2H, m), 6.07(1H, d, J=7.5 Hz), 7.04(1H, dd,J=3.6 and 5.4 Hz), 7.11(1H, d, J=3.9 Hz), 7.24(1H, dd, J=1.2 and 3.6Hz), 7.28(1H, dd, J=1.2 and 5.4 Hz), 7.42(1H, d J=3.9 Hz). IR(CHCl₃):3511, 3445, 3428, 3113, 3073, 2667, 1708, 1643, 1521, 1498, 1455 cm⁻¹.[α]_(D) ²⁵+89.5±1.30°(c=1.005, MeOH) Anal. (C₂₃H₂₇NO₃S₂.0.1H₂O)Calcd.(%): C, 64.04; H, 6.36; N, 3.25; S, 14.86. Found(%): C, 63.93; H,6.39; N, 3.46; S, 14.61.

Compound Number I-44

mp.146–147° C.; ¹H-NMR(CDCl₃) δ: 1.10(1H, m), 1.24–1.31(2H, m),1.46–1.51(2H, m), 1.61–1.82(4H, m), 2.00–2.24(5H, m), 2.37(2H, t, J=7.2Hz), 2.37(3H, s), 2.56(1H, m), 3.85(1H, m), 5.31–5.45(2H, m), 6.06(1H,d, J=6.9 Hz), 7.20 and 7.51(each 2H, each d, each J=9.0 Hz), 7.21 and7.48(each 1H, each d, each J=3.9 Hz). IR(CHCl₃): 3517, 3445, 3428, 1740,1708, 1642, 1542, 1518, 1498, 1451 cm⁻¹. [α]_(D) ²⁶+89.3±1.3°(c=1.009,MeOH) Anal. (C₂₆H₃₁NO₃S) Calcd.(%): C, 71.36; H, 7.14; N, 3.20; S, 7.33.Found(%): C, 71.51; H, 7.10; N, 3.20; S, 7.33.

Compound Number I-45

mp.110–116° C. ¹H-NMR(CDCl₃) δ: 1.10(1H, m), 1.24–1.31(2H, m),1.46–1.51(2H, m), 1.61–1..83(4H, m), 2.00–2.25(5H, m), 2.37(2H, t, J=7.2Hz), 2.56(1H, m), 3.84(3H, s), 3.85(1H, m), 5.31–5.45(2H, m), 6.04(1H,d, J=7.5 Hz), 6.93 and 7.55(each 2H, each d, each J=8.7 Hz), 7.15 and7.46 (each 2H, each d, each J=4.2 Hz). IR(CHCl₃): 3515, 3445, 3428,1740, 1708, 1640, 1608, 1541, 1499, 1453, 1178 cm⁻¹. [α]_(D)²⁶+88.0±1.3°(c=1.010, MeOH) Anal. (C₂₆H₃₁NO₄S) Calcd.(%): C, 68.85; H,6.89; N, 3.09; S, 7.07. Found(%): C, 68.87; H, 6.82; N, 3.11; S, 7.19.

Compound Number I-46

mp.124–125° C.,; ¹H-NMR(CDCl₃) δ: 1.10(1H, m), 1.24–1.32(2H, m),1.46–1.51(2H, m), 1.61–1.82(4H, m), 2.00–2.24(5H, m), 2.37(2H, t, J=7.2Hz), 2.56 (1H, m), 3.85(1H, m), 5.32–5.45(2H, m), 6.06(1H, d, J=7.2 Hz),7.10 (2H, t, J=8.7 Hz), 6.19 and 7.47(each 1H, each d, each J=3.6 Hz),7.56–5.60 (2H, m). IR(CHCl₃): 3516, 3445, 3428, 2672, 1740, 1708, 1643,1542, 1519, 1498, 1452 cm⁻¹. [α]_(D) ²⁶+83.3±1.2°(c=1.005, MeOH) Anal.(C₂₅H₂₈FNO₃S) Calcd.(%): C, 68.00; H, 6.39; N, 3.17; F, 4.30; S, 7.26.Found(%): C, 67.90; H, 6.34; N, 3.25; F, 4.31; S, 7.20.

Compound Number I-47

¹H-NMR(CDCl₃) δ: 1.10(1H, m), 1.18–1.32(2H, m), 1.38–1.48(2H, m),1.56–1.76(4H, m), 2.00–2.18(5H, m), 2.35(2H, t, J=7.2 Hz), 2.53(1H, m),3.81 (1H, m), 5.31–5.43(2H, m), 6.32(1H, d, J=7.5 Hz), 7.11(1H, dd,J=3.9 and 5.1 Hz), 7.4 and 7.62(each 1H, each d, each J=3.9 Hz),7.70(1H, dd, J=1.5 and 5.1 Hz), 7.74(1H, dd, J=1.5 and 3.9 Hz).IR(CHCl₃): 3516, 3442, 3378, 1708, 1655, 1530, 1504, 1336, 1153 cm⁻¹.[α]_(D) ²⁵+74.3±1.1°(c=1.000, MeOH) Anal. (C₂₃H₂₇NO₅S₃.0.1H₂O)Calcd.(%): C, 55.76; H, 5.53; N, 2.83; S, 19.41. Found(%): C, 55.49; H,5.64; N, 3.09; S, 19.32.

Compound Number I-48

mp.112–115° C. ¹H-NMR(CDCl₃) δ: 1.13–1.30(3H, m), 1.34–1.45 (2H, m),1.50–1.82(4H, m), 1.94–2.27(5H, m), 2.34(2H, t, J=7.2 Hz), 2.56 (1H, m),3.74(1H, m), 5.22(2H, s), 5.31–5.50(2H, m), 6.64(1H, d, J=6.6 Hz), 6.84(1H, (1, J=3.9 Hz), 6.93 and 7.05(each 1H, each s), 7.47(1H, d, J=3.9Hz), 7.66(1H, s). IR(Nujol): 3339, 3102, 2464, 1691, 1635, 1622, 1551,1288 cm⁻¹. [α]_(D) ²⁵+71.2±1.1°(c=1.005, MeOH) Anal. (C₂₃H₂₉N₃O₃S)Calcd.(%): C, 64.61; H, 6.84; N, 9.83; S, 7.50. Found(%): C, 64.54; H,6.85; N, 9.78; S, 7.42.

Compound Number I-49

¹H-NMR(CDCl₃) δ: 1.08(1H, m), 1.16–1.30(2H, m), 1.38–1.47(2H, m),1.54–1.77(4H, m), 1.98–2.20(5H, m), 2.34(2H, t, J=7.2 Hz), 2.52(1H, m),3.79 (1H, m), 5.30–5.42(2H, m), 5.47(2H, s), 6.16(1H, d, J=6.9 Hz),6.30(1H, t, J=2.1 Hz) 6.94 and 7.41(each 1H, each d, each J=3.6 Hz),7.47 and 7.57 (each 1H, each d, each J=2.1 Hz). IR(CHCl₃): 3510, 3444,3426, 1709, 1646, 1546, 1512 cm⁻¹. [α]_(D) ²⁵+68.6±1.1°(c=1.011, MeOH)Anal. (C₂₃H₂₉N₃O₃S.0.1H₂O) Calcd.(%): C, 64.34; H, 6.85; N, 9.79; S,7.47. Found(%): C, 64.10; H, 6.93; N, 9.90; S, 7.52.

Compound Number I-50

mp.126–128° C.; ¹H-NMR(CDCl₃) δ: 1.12(1H, m), 1.18–1.33(2H, m),1.40–1.50(2H, m), 1.55–1.78(4H, m), 2.00–2.21(5H, m), 2.54(1H, m),3.87(1H, m), 5.30–5.44(2H, m), 6.43(1H, d, J=6.6 Hz), 7.48–7.62(3H, m),7.83–7.95(5H, m). IR(Nujol): 3284, 3058, 2669, 1701, 1641, 1546, 1326,1294, 1160 cm⁻¹. [α]hd D²⁵+77.2±1.2°(c=1.007, MeOH) Anal. (C₂₇H₃₁NO₅S)Calcd.(%): C, 67.34; H, 6.49; N, 2.91; S, 6.66. Found(%): C, 67.20; H,6.38; N, 2.88; S, 6.58.

Compound Number I-51

mp.103–107° C. ¹H-NMR(CDCl₃) δ: 1.14(1H, m), 1.18–1.33(2H, m),1.40–1.50(2H, m), 1.54–1.77(4H, m), 2.00–2.20(5H, m), 2.34(2H, t, J=7.2Hz), 2.54(1H, m), 3.85(3H, s), 3.86(1H, m), 5.30–5.45(2H, m), 6.48(1H,d, J=6.9 Hz), 6.96(2H, m), 7.81–7.91(6H, m). IR(Nujol): 3273, 3067,2669, 1702, 1639, 1560, 1548, 1323, 1301, 1274, 1156 cm⁻¹. [α]_(D)²⁵+75.4±1.2°(c=1.002, MeOH) Anal. (C₂₈H₃₃NO₆S) Calcd.(%): C, 65.73; H,6.50; N, 2.74; S, 6.27. Found(%): C, 65.50; H, 6.46; N, 2.82; S, 6.25.

Compound Number I-52

¹H-NMR(CDCl₃) δ: 1.17(1H, m), 1.26–1.34(2H, m), 1.47–1.53(2H, m),1.60–1.76(4H, m), 2.04–2.21(5H, m), 2.36(2H, t, J=7.2 Hz), 2.60(1H, m),3.91(1H, m), 5.32–5.47(2H, m), 6.46(1H, d, J=8.4 Hz), 7.17(1H, dd, J=3.9and 5.1 Hz), 7.61(1H, dd, J=1.2 and 3.9 Hz), 7.76(1H, dd, J=1.2 and 5.1Hz), 7.87(4H, s-like). IR(CHCl₃): 3518, 3444, 2663, 1708, 1638, 1517,1494, 1414 cm⁻¹. [α]_(D) ²⁵+86.6±1.3°(c=1.008, MeOH) Anal. (C₂₆H₂₉NO₄S)Calcd.(%): C, 69.15; H, 6.47; N, 3.10; S, 7.10. Found(%): C, 68.86; H,6.70; N, 3.15; S, 6.95.

Compound Number I-53

mp.144–145° C.; ¹H-NMR(CDCl₃) δ: 1.20–2.54(16H, m), 2.62(1H, m), 3.69(3H, s), 5.35–5.56(2H, m), 6.36 and 7.17(each 2H, each t, each J=2.4Hz), 6.66(1H, d, J=6.3 Hz), 8.05 and 8.07(each 1H, each d, each J=1.5Hz). IR(Nujol): 3509, 3406, 3146, 3110, 1728, 1708, 1653, 1535, 1375,1189, 1166 cm⁻¹. [α]_(D) ²⁵+67.9±1.1°(c=1.007, MeOH) Anal.(C₂₃H₂₈N₂O₅S₂) Calcd.(%): C, 57.96; H, 5.92; N, 5.88; S, 13.45.Found(%): C, 58.19; H, 5.95; N, 5.75; S, 13.09.

Compound Number I-54

¹H-NMR(CDCl₃) δ: 1.22–2.57(16H, m), 2.68(1H, m), 3.66(3H, s), 5.37–5.63(2H, m), 6.20, 6.35, 6.74 and 6.87(each 2H, each t, each J=2.4 Hz), 6.92(1H, d, J=5.4 Hz), 8.27(1H, s). IR(CHCl₃): 3402, 3143, 3108, 1725, 1710,1650, 1516, 1375 cm⁻¹. [α]_(D) ²⁶+70.0±1.1°(c=1.006, MeOH) Anal.(C₂₇H₃₁N₃O₅S₂.0.3H₂O) Calcd.(%): C, 59.28; H, 5.82; N, 7.68; S, 11.72.Found(%): C, 59.28; H, 5.77; N, 5.58; S, 11.68.

Compound Number I-55

¹H-NMR(CDCl₃) δ: 1.10(1H, m), 1.18–1.31(2H, m), 1.40–1.45(2H, m),1.57–1.74(4H, m), 2.00–2.10(5H, m), 2.35(2H, t, J=7.2 Hz), 2.38(3H, s),2.52 (1H, m), 3.80(1H, m), 5.31–5.43(2H, m), 5.99(1H, m), 6.20(1H, t,J=3.3 Hz), 6.30(1H, d, J=6.91 Hz), 7.18(1H, dd, J=1.8 and 3.3 Hz), 7.40and 7.53(each 1H, each d, each J=3.9 Hz). IR(CHCl₃): 3513, 3442, 3149,3100, 1708, 1657, 1530, 1504, 1375, 1183, 1161 cm⁻¹. [α]_(D)²⁷+70.3±1.5°(c=0.730, MeOH) Anal. (C₂₄H₃₀N₂O₅S₂.0.4H₂O) Calcd.(%): C,57.90; H, 6.24; N, 5.63; S, 12.88. Found(%): C, 58.08; H, 6.28; N, 5.77;S, 12.54.

Compound Number I-56

¹H-NMR((d₆-DMSO) δ: 1.06–1.59(9H, m), 1.93–2.07(5H, m), 2.21(2H, t,J=7.2 Hz), 2.35(1H, m), 3.65(1H, m), 5.30–5.41(2H, m), 6.90 and 7.69(each 1H, each d, each J=4.2 Hz), 7.55–7.64(3H, m), 7.99–8.04(3H, m),11.73 (1H, s), 12.01(1H, brs). IR (KBr): 3562, 1708, 1616, 1564, 1523,1454, 1295 cm⁻¹. [α]_(D) ²⁷+71.2±1.1°(c=1.000, MeOH) Anal.(C₂₆H₃₀N₂O₄S.0.2H₂O) Calcd.(%): C, 66.42; H, 6.52; N, 5.96; S, 6.82.Found(%): C, 66.43; H, 6.32; N, 6.17; S, 6.75.

Compound Number I-57

¹H-NMR(d₆-DMSO) δ: 1.05–1.56(9H, m), 1.91–2.05(5H, m), 2.19(2H, t, J=7.2Hz), 2.29(1H, m), 3.56(1H, m), 5.28–5.38(2H, m), 6.54 and 7.56(each 1H,each d, each J=4.2 Hz), 7.59–7.62(3H, m), 7.76–7.79(2H, m), 8.06(1H, d,J=6.9 Hz), 11.10(1H, s), 11.99(1H, brs). IR(KBr): 3384, 3084, 1707,1616, 1553, 1523, 1459, 1350, 1322, 1161 cm⁻¹. [α]_(D)²⁷+62.4±1.0°(c=1.005, MeOH) Anal. (C₂₅H₃₀N₂O₅S₂.0.2H₂O) Calcd.(%): C,59.31; H, 6.05; N, 5.53; S, 12.66. Found(%): C, 59.36; H, 5.75; N, 5.55;S, 12.38.

Compound Number I-58

¹H-NMR(CDCl₃) δ: 1.07(1H, m), 1.17–1.33(2H, m), 1.36–1.50(2H, m),1.54–1.75(4H, m), 2.00–2.20(5H, m), 2.35(2H, t, J=7.2 Hz), 2.45(3H, s),2.52 (1H, m), 3.80(1H, m), 5.31–5.43(2H, m), 6.12(1H, d, J=7.5 Hz), 6.32and 7.18(each 2H, each t, each J=2.4 Hz), 7.22(1H, s). IR(CHCl₃): 3316,3442, 3145, 2668, 1708, 1657, 1545, 1509, 1455, 1375, 1190, 1165, 1057cm⁻¹. [α]_(D) ²⁶+75.8±1.2°(c=1.002, MeOH) Anal. (C₂₄H₃₀N₂O₅S₂.0.1H₂O)Calcd.(%): C, 58.54; H, 6.18; N, 5.69; S, 13.02. Found(%): C, 58.35; H,6.29; N, 5.74; S, 12.92.

Compound Number I-59

¹H-NMR(CDCl₃) δ: 1.05(1H, m), 1.16–1.30(2H, m), 1.38–1.48(2H, m),1.53–1.79(4H, m), 1.98–2.17(5H, m), 2.34(2H, t, J=7.2 Hz), 2.50(1H, m),3.79(1H, m), 5.30–5.42(2H, m), 6.00(1H, d, J=7.5 Hz), 7.01(1H, dd, J=3.6and 5.4 Hz), 7.03(1H, d, J=3.9 Hz), 7.29(1H, dd, J=1.2 and 3.6 Hz),7.33(1H, d, J=3.9) 7.43(1H, dd, J=1.2 and 5.4 Hz). IR(CHCl₃): 3517,3444, 3426, 2670, 1708, 1645, 1530, 1499, 1421, 1318 cm⁻¹. [α]_(D)²⁶+70.8±1.1°(c=1.018, MeOH) Anal. (C₂₃H₂₇NO₃S₃) Calcd.(%): C, 59.84; H,5.89; N, 3.03; S, 20.84. Found(%): C, 59.73; H, 5.99; N, 3.15; S, 20.70.

Compound Number I-60

¹H-NMR(CDCl₃) δ: 1.07(1H, m), 1.17–1.32(2H, m), 1.40–1.50(2H, m),1.56–1.80(4H, m), 1.99–2.21(5H, m), 2.34(2H, t, J=7.2 Hz), 2.54(1H, m),3.85 (1H, m), 5.29–5.42(2H, m), 6.20(1H, d, J=6.9 Hz), 7.23–7.45(7H, m),7.55 (2H, d, J=8.1 Hz). IR(CHCl₃): 3516, 3447, 2667, 1708, 1651, 1596,1514, 1481 cm⁻¹. [α]_(D) ²⁶+89.1±1.3°(c=1.006, MeOH) Anal.(C₂₇H₃₁NO₃S.0.2H₂O) Calcd.(%): C, 71.56; H, 6.98; N, 3.09; S, 7.07.Found(%): C, 71.39; H, 6.97; N, 3.16; S, 6.94.

Compound Number I-61

¹H-NMR(CDCl₃) δ: 1.06(1H, m), 1.18–1.31(2H, m), 1.41–1.50(2H, m),1.55–1.80(4H, m), 1.99–2.20(5H, m), 2.35(2H, t, J=7.2 Hz), 2.52(1H, m),3.82(1H, m), 5.31–5.43(2H, m), 5.97(1H, d, J=6.6 Hz), 6.45(1H, d, J=4.2Hz), 7.11–7.20(3H, m), 7.28(1H, d, J=4.2 Hz), 7.33–7.40(2H, m).IR(CHCl₃): 3515, 3445, 3427, 2667, 1740, 1708, 1640, 1506, 1475 cm⁻¹.[α]_(D) ²⁷+71.3±1.1°(c=1.002, MeOH) Anal. (C₂₅H₂₉NO₄S) Calcd.(%): C,68.31; H, 6.65; N, 3.19; S, 7.29. Found(%): C, 68.41; H, 6.87; N, 3.22;S, 7.35.

Compound Number I-62

¹H-NMR(CDCl₃) δ: 1.14(1H, m), 1.20–1.35(2H, m), 1.42–1.54(2H, m),1.57–1.77(4H, m), 2.00–2.23(5H, m), 2.35(2H, t, J=7.2 Hz), 2.58(1H, m),3.88(1H, m), 5.32–5.46(2H, m), 6.31 and 7.19(each 2H, each t, each J=2.4Hz), 6.33(1H, d, J=7.5 Hz), 7.77(1H, dd, J=1.8 and 8.4 Hz), 7.77(1H, s),7.87(1H, d, J=8.4 Hz), 8.38(1H, d, J=1.8 Hz). IR(CHCl₃): 3514, 3442,3422, 3144, 2670, 1708, 1654, 1525, 1375, 1193, 1171 cm⁻¹. [α]_(D)²⁶+^(89.8±1.3)°(c=1.000, MeOH) Anal. (C₂₇H₃N₂O₅S₂) Calcd.(%): C, 61.58;H, 5.74; N, 5.32; S, 12.17. Found(%): C, 61.42; H, 5.86; N, 5.57; S,11.98.

Compound Number I-63

mp.180–181° C.; ¹H-NMR(CDCl₃) δ: 1.04(1H, m), 1.22–1.30(2H, m),1.41–1.46 (2H, m), 1.59–1.82(4H, m), 1.94–2.16(3H, m), 2.25–2.37(2H, m),2.42 (2H, t, J=6.9 Hz), 2.52(1H, m), 2.52(3H, s), 3.79(1H, m),5.41–5.59(2H, m), 5.73(1H, d, J=6.6 Hz), 7.48–7.53(2H, m), 7.60(1H, m),8.07–8.10(2H, m). IR(Nujol): 3372, 3173, 3053, 2544, 1690, 1672, 1632,1559, 1496, 1362, 1317 cm⁻¹. [α]_(D) ²⁸+77.7±1.2°(c=1.007, MeOH) Anal.(C₂₆H₃₁N₃O₄S) Calcd.(%): C, 64.84; H, 6.49; N, 8.72; S, 6.66. Found(%):C, 64.66; H, 6.31; N, 8.73; S, 6.65.

Compound Number I-64

¹H-NMR(d₆-DMSO) δ: 1.07(1H, m), 1.28–1.58(8H, m), 1.91–2.08(5H, m),2.20(2H, t, J=7.2 Hz), 2.31(3H, s), 2.32(1H, s), 3.96(1H, m),5.28–5.40(2H, m), 7.52–7.62(3H, m), 7.80–7.83(2H, m), 7.94(1H, d, J=6.9Hz). IR(Nujol): 3316, 3161, 3106, 2677, 1709, 1629, 1531, 1284, 1142cm⁻¹. [α]_(D) ²⁷+76.2±1.2°(c=1.002, MeOH) Anal. (C₂₅H₃₁N₃O₅S₂.0.1H₂O)Calcd.(%): C, 57.80; H, 6.05; N, 8.09; S, 12.34. Found(%): C, 57.59; H,6.15; N, 8.10; S, 12.57.

Compound Number I-65

¹H-NMR(CDCl₃) δ: 1.28–1.31(2H, m), 1.47(2H, brs), 1.56–1.84(4H, m),1.94–2.30(5H, m), 2.39(2H, t, J=6.9 Hz), 2.62(1H, s), 2.63(3H, s),3.77(1H, m), 5.35–5.67(2H, m), 6.42(1H, d, J=6.3 Hz), 7.29–7.43(3H, m),7.46(1H, s), 7.72(2H, d, J=7.2 Hz). IR(CHCl₃): 3517, 3421, 3350, 3150,2538, 1708, 1651, 1590, 1512, 1474, 1442, 1164 cm⁻¹. [α]_(D)²⁸+100.8±1.4°(c=1.002, MeOH) Anal. (C₂₇H₃₁N₃O₃S.0.5H₂O) Calcd.(%): C,66.64; H, 6.63; N, 8.63; S, 6.59. Found(%): C, 66.55; H, 6.59; N, 8.68;S, 6.76.

Compound Number I-66

¹H-NMR(CDCl₃) δ: 1.08(1H, m), 1.19–1.33(2H, m), 1.42–1.50(2H, m),1.58–1.79(4H, m), 2.01–2.22(5H, m), 2.35(2H, t, J=7.2 Hz), 2.55(1H, m),3.86(1H, m), 4.37(2H, s), 5.30–5.43(2H, m), 6.19(1H, d, J=7.5 Hz),6.90(1H, dd, J=3.6 and 5.1 Hz), 6.93(1H, m), 7.17(1H, dd, J=1.2 and 5.1Hz), 7.33 and 7.65(each 2H, each d, J=8.4 Hz). IR(CHCl₃): 3518, 3447,2665, 1708, 1651, 1596, 1515, 1484 cm⁻¹. [α]_(D) ²⁶+82.4±1.4°(c=0.900,MeOH) Anal. (C₂₆H₃₁NO₃S₂.0.1H₂O) Calcd.(%): C, 66.24; H, 6.67; N, 2.97;S, 13.60. Found(%): C, 66.14; H, 6.72; N, 2.96; S, 13.53.

Compound Number I-67

¹H-NMR(CDCl₃) δ: 1.16(1H, m), 1.21–1.34(2H, m), 1.43–1.52(2H, m),1.57–1.76(4H, m), 2.04–2.22(5H, m), 2.35(2H, t, J=7.2 Hz), 2.56(1H, m),3.89 (1H, m), 4.53(2H, s), 5.33–5.48(2H, m), 6.58(1H, d, J=6.9 Hz),6.83(1H, dd, J=1.2 and 3.9 Hz), 6.93(1H, dd, J=3.9 and 5.1 Hz), 7.28(1H,dd, J=1.2 and 5.1 Hz), 7.65 and 7.81(each 2H, each d, J=8.4 Hz).IR(CHCl₃): 3518, 3442, 3373, 2666, 1708, 1658, 1516, 1483, 1323, 1153m⁻¹. [α]_(D) ²⁶+69.6±1.1°(c=1.003, MeOH) Anal. (C₂₆H₃₁NO₅S₂.0.5H₂O)Calcd.(%): C, 61.15; H, 6.32; N, 2.74; S, 12.56. Found(%): C, 66.16; H,6.25; N, 2.90; S, 12.57.

Compound Number I-68

¹H-NMR(CDCl₃) δ: 1.13(1H, m), 1.20–1.32(2H, m), 1.38–1.50(2H, m),1.54–1.77(4H, m), 1.98–2.20(5H, m), 2.35(2H, t, J=7.2 Hz), 2.53(1H, m),3.80 (1H, m), 5.31–5.46(2H, m), 6.47(1H, d, J=7.5 Hz), 6.87(1H, dd,J=1.5 and 3.6 Hz), 3.84(1H, dd, J=3.6 and 5.4 Hz), 7.03(1H, dd, J=1.5and 5.4 Hz), 7.33 and 7.38(each 1H, each d, each J=3.9 Hz), 7.90(1H,br). IR(CHCl₃): 3510, 3440, 3358, 3109, 1708, 1647, 1533, 1505, 1364,1331, 1161 cm⁻¹. [α]₄₃₆ ²⁹+151.3±1.9°(c=1.010, MeOH) Anal.(C₂₃H₂₈N₂O₅S₃.0.1H₂O) Calcd.(%): C, 54.12; H, 5.57; N, 5.49; S, 18.84.Found(%): C, 53.84; H, 5.46; N, 5.38; S, 18.62.

Compound Number I-69

¹H-NMR(CDCl₃) δ: 1.20(1H, m), 1.26–1.38(2H, m), 1.42–1.52(2H, m),1.57–1.76(4H, m), 2.00–2.24(5H, m), 2.34(2H, t, J=7.2 Hz), 2.53(1H, m),3.88 (1H, m), 5.31–5.49(2H, m), 6.63(1H, dd, J=1.2 and 3.9 Hz), 6.69(1H,d, J=7.5 Hz), 6.77(1H, dd, J=3.9 and 5.4 Hz), 6.98(1H, dd, J=1.2 and 5.4Hz), 7.66 and 7.76(each 2H, each d, each J=8.4 Hz). IR(CHCl₃): 3509,3439, 3363, 3111, 1707, 1651, 1520, 1328, 1167 cm⁻¹. [α]₄₃₆²⁹+155.7±2.0°(c=1.003, MeOH) Anal. (C₂₅H₃₀N₂O₅S₃.0.3H₂O) Calcd.(%): C,59.10; H, 6.07; N, 5.51; S, 12.62. Found(%): C, 59.00; H, 5.95; N, 5.51;S, 12.46.

Compound Number I-70

mp.187–188° C.; ¹H-NMR(d₆-DMSO) δ: 1.16–1.62(9H, m), 1.90–2.14(5H, m),2.21(2H, t, J=7.2 Hz), 2.38(1H, m), 3.66(1H, m), 5.27–5.41(2H, m),7.10–7.15 (1H, m), 7.34–7.39(2H, m), 7.42–7.75(2H, m), 7.91 and7.99(each 1H, each d, each J=3.9 Hz), 8.04(1H, d, J=6.6 Hz), 10.32(1H,s), 12.02(1H, s). IR(Nujol): 3316, 3075, 2678, 1704, 1635, 1614, 1544,1323 cm⁻¹. [α]_(D) ²⁸+83.3±1.2°(c=1.003, MeOH) Anal. (C₂₆H₃₀N₂O₄S)Calcd.(%): C, 66.93; H, 6.48; N, 6.00; S, 6.87. Found(%): C, 67.04; H,6.45; N, 5.98; S, 6.96.

Compound Number I-71

mp.192–194° C.; ¹H-NMR(d₆-DMSO) δ: 1.16–1.62(9H, m), 1.90–2.14(5H, m),2.21(2H, t, J=7.2 Hz), 2.37(1H, m), 3.65(1H, m), 5.29–5.41(2H, m),7.18–7.24 (2H, m), 7.33–7.78(2H, m), 7.91 and 7.97(each 1H, each d, eachJ=3.9 Hz), 8.04(1H, d, J=6.9 Hz), 10.38(1H, s), 12.01(1H, s). IR(Nujol):3322, 3278, 3150, 3098, 3077, 2678, 1704, 1635, 1615, 1546, 1521, 1508,1322 cm⁻¹. [α]_(D) ²+83.3±1.2°(c=1.000, MeOH) Anal. (C₂₆H₂₉FN₂O₄S)Calcd.(%): C, 64.44; H, 6.03; N, 5.78; F, 3.92; S, 6.62. Found(%): C,64.36; H, 6.00; N, 5.81; F, 3.94; S, 6.46.

Compound Number I-72

mp.192–193° C.; ¹H-NMR(d₆-DMSO) δ: 1.16–1.62(9H, m), 1.92–2.14 (5H, m),2.21(2H, t, J=7.2 Hz), 2.37(1H, m), 3.66(1H, m), 3.75(3H, s),5.30–5.41(2H, m), 6.94 and 7.63(each 2H, each d-like), 7.89 and7.94(each 1H, each d, each J=3.9 Hz), 8.38(1H, d, J=6.9 Hz), 10.21(1H,s), 12.01(1H, s). IR(Nujol): 3316, 3075, 2678, 1704, 1635, 1614, 1544,1323 cm⁻¹. [α]_(D) ²⁷+81.6±1.2°(c=1.000, MeOH) Anal. (C₂₇H₁₃₂N₂O₅S)Calcd.(%): C, 65.30; H, 6.49; N, 5.64; S, 6.46. Found(%): C, 65.19; H,6.49; N, 5.45; S, 6.31.

Compound Number I-73

¹H-NMR(CDCl₃) δ: 1.14(1H, m), 1.18–1.32(2H, m), 1.40–1.78(6H, m),1.94–2.20 (5H, m), 2.35(2H, t, J=7.2 Hz), 2.51(1H, m), 3.80(1H, m),3.81(6H, s), 3.82(3H, s), 5.30–5.44(2H, m), 6.56(1H, d, J=7.2 Hz),6.97(2H, s), 7.47 and 7.58(each 1H, each d, each J=3.9 Hz), 8.43(1H, s).IR(CHCl₃): 3515, 3438, 3317, 1708, 1650, 1607, 1537, 1508, 1454, 1412,1131 cm⁻¹. [α]_(D) ²⁷+75.8±1.2°(c=1.009, MeOH) Anal.(C₂₉H₃₆N₂O₇S.0.4H₂O) Calcd.(%): C, 61.77; H, 6.58; N, 4.97; S, 5.69.Found(%): C, 61.74; H, 6.64; N, 4.89; S, 5.89.

Compound Number I-74

¹H-NMR(CDCl₃) δ: 1.10(1H, m), 1.20–1.33(2H, m), 1.43–1.52(2H, m),1.57–1.78(4H, m), 2.00–2.21(5H, m), 2.36(2H, t, J=7.2 Hz), 2.55(1H, m),3.85(1H, m), 5.32–5.45(2H, m), 6.09(1H, d, J=6.9 Hz), 6.32 and 7.00(each2H, each t, each J=2.1 Hz), 6.81 and 7.34(each 1H, each d, each J=3.9Hz). IR(CHCl₃): 3515, 3445, 3109, 2678, 1740, 1708, 1642, 1507, 1489cm⁻¹. [α]_(D) ²⁶+83.5±1.2°(c=1.007, MeOH) Anal. (C₂₃H₂₈N₂O₃S) Calcd.(%):C, 66.96; H, 6.84; N, 6.79; S, 7.77. Found(%): C, 66.66; H, 6.74; N,6.74; S, 7.61.

Compound Number I-75

¹H-NMR(CDCl₃) δ: 1.09(1H, m), 1.20–1.32(2H, m), 1.39–1.49(2H, m),1.57–1.66(4H, m), 2.01–2.22(5H, m), 2.35(2H, t, J=7.2 Hz), 2.56(1H, m),3.88(1H, m), 3.95(2H, s), 5.30–5.44(2H, m), 6.27(1H, d, J=7.5 Hz),6.89–6.91(2H, m), 7.32(1H, dd, J=2.4 and 3.9 Hz), 7.19 and 7.66(each 2H,each d, J=8.4 Hz). IR(CHCl₃): 3516, 3447, 2670, 1708, 1651, 1523, 1496m⁻¹. [α]_(D) ²⁶+71.8±1.1°(c=1.016, MeOH) Anal. (C₂₆H₃NO₃S₂.0.1H₂O)Calcd.(%): C, 66.24; H, 6.67; N, 2.97; S, 13.60. Found(%): C, 66.36; H,6.67; N, 3.27; S, 13.62.

Compound Number I-76

mp.135–136° C.; ¹H-NMR(CDCl₃) δ: 1.12(1H, m), 1.22–1.33(2H, m),1.43–1.51(2H, m), 1.59–1.78(4H, m), 2.03–2.22(5H, m), 2.35(2H, t, J=7.2Hz), 2.56 (1H, m), 3.87(1H, m), 4.44(2H, s), 5.31–5.45(2H, m), 6.30(1H,d, J=7.2 Hz), 7.08(1H, dd, J=3.9 and 5.1 Hz), 7.23(2H, d, J=8.4 Hz),7.40(1H, dd, J=1.5 and 3.9 Hz), 7.69–7.71(3H, m). IR(CHCl₃): 3516, 3445,3096, 2665, 1708, 1655, 1523, 1496, 1403, 1327, 1152, 1127 m⁻¹. [α]_(D)²⁶+65.0±1.1°(c=1.000, MeOH) Anal. (C₂₆H₃₁NO₅S₂.0.2H₂O) Calcd.(%): C,61.81; H, 6.26; N, 2.77; S, 12.69. Found(%): C, 61.76; H, 6.20; N, 2.90;S, 12.57.

Compound Number I-77

mp.215–217° C. ¹H-NMR(d₆-DMSO) δ: 1.16–1.62(9H, m), 1.90–2.14 (5H, m),2.21(2H, t, J=7.2 Hz), 2.38(1H, m), 3.66(1H, m), 5.29–5.41 (2H, m),6.91–6.94(2H, m), 7.05(1H, dd, J=2.4 and 4.2 Hz), 7.93 and 7.96 (each1H, each d, each J=4.2 Hz), 8.43(1H, d, J=6.6 Hz), 10.67(1H, br), 12.01(1H, br). IR(Nujol): 3315, 3222, 3097, 3049, 2672, 1705, 1621, 1548,1504, 1311 cm⁻¹. [α]_(D) ²⁷+88.2±1.3°(c=1.009, MeOH) Anal.(C₂₄H₂₈N₂O₄S₂) Calcd.(%): C, 60.99; H, 5.97; N, 5.93; S, 13.57.Found(%): C, 60.94; H, 5.74; N, 5.91; S, 13.61.

Compound Number I-78

¹H-NMR(CDCl₃) δ: 1.09(1H, m), 1.18–1.31(2H, m), 1.40–1.47(2H, m),1.57–1.73(4H, m), 2.00–2.12(5H, m), 2.31(2H, t, J=7.2 Hz), 2.56(1H, m),3.79 (1H, m), 4.70(2H, s), 5.30–5.45(2H, m), 6.26–6.30(2H, m), 6.34(1H,d, J=6.9 Hz), 7.22(1H, dd, J=1.8 and 3.3 Hz), 7.41 and 7.62(each 1H,each d, each J=4.2 Hz). IR(CHCl₃): 3589, 3516, 3441, 3355, 3100, 1708,1656, 1530, 1504, 1377, 1180, 1147 cm⁻¹. [α]_(D)^(26.5)+70.8±1.1°(c=1.009, MeOH) Anal. (C₂₄H₃₀N₂O₆S₂.0.2H₂O) Calcd.(%):C, 56.50; H, 6.01; N, 5.49; S, 12.57. Found(%): C, 56.43; H, 6.02; N,5.61; S, 12.47.

Compound Number I-79

¹H-NMR(CDCl₃) δ: 1.06(1H, m), 1.16–1.30(2H, m), 1.38–1.50(2H, m),1.54–1.77(4H, m), 1.98–2.18(5H, m), 2.35(2H, t, J=7.2 Hz), 2.51(1H, m),3.80(1H, m), 5.30–5.42(2H, m), 6.03(1H, d, J=7.2 Hz), 7.04–7.06(2H, m),7.32–7.35(2H, m), 7.37(1H, d, J=3.6 Hz). IR(CHCl₃): 3509, 3444, 3426,3110, 2667, 1708, 1645, 1530, 1499, 1421 cm⁻¹. [α]_(D)^(26.5)+69.5±1.1°(c=1.001, MeOH) Anal. (C₂₃H₂₇NO₃S₃.0.1H₂O) Calcd.(%):C, 59.61; H, 5.92; N, 3.02; S, 20.76. Found(%): C, 59.66; H, 5.90; N,3.15; S, 20.52.

Compound Number I-80

¹H-NMR(CDCl₃) δ: 1.10(1H, m), 1.17–1.32(2H, m), 1.38–1.48(2H, m),1.54–1.77(4H, m), 2.00–2.20(5H, m), 2.35(2H, t, J=7.2 Hz), 2.53(1H, m),3.81(1H, m), 5.31–5.43(2H, m), 6.31(1H, d, J=7.2 Hz), 7.37–7.44(3H, m),7.61(1H, d, J=3.9 Hz), 8.15(1H, dd, J=1.2 and 3.0 Hz). IR(CHCl₃): 3517,3441, 3371, 3114, 1708, 1655, 1530, 1504, 1331, 1152 cm⁻¹. [α]_(D)^(26.5)+73.9±1.1°(c=1.001, MeOH) Anal. (C₂₃H₂₇NO₅S₃.0.3H₂O) Calcd.(%):C, 55.35; H, 5.57; N, 2.81; S, 19.28 Found(%): C, 55.47; H, 5.50; N,2.80; S, 19.09.

Compound Number I-81

¹H-NMR(CDCl₃) δ: 1.05(1H, m), 1.16–1.30(2H, m), 1.38–1.48(2H, m),1.54–1.77 (4H, m), 1.98–2.17(5H, m), 2.34(2H, t, J=7.2 Hz), 2.46(3H, d,J=0.9 Hz), 2.50(1H, m), 3.79(1H, m), 5.29–5.41(2H, m), 5.99(1H, d, J=7.2Hz), 6.67(1H, m), 6.99, 7.10 and 7.32(each 1H, each d, each J=3.9 Hz).IR(CHCl₃): 3517, 3445, 3426, 2668, 1708, 1644, 1530, 1499, 1420, cm⁻¹.[α]_(D) ^(26.5)+66.1±1.1°(c=1.002, MeOH) Anal. (C₂₄H₂₉NO₃S₃.0.1H₂O)Calcd.(%): C, 60.37; H, 6.16; N, 2.93; S, 20.15. Found(%): C, 60.21; H,6.10; N, 2.90; S, 20.45.

Compound Number I-82

¹H-NMR(CDCl₃) δ: 1.11(1H, m), 1.18–1.32(2H, m), 1.38–1.50(2H, m),1.54–1.74. (4H, m), 2.00–2.20(5H, m), 2.35(2H, t, J=7.2 Hz), 2.53(4H, dand m, J=0.6 Hz), 3.80(1H, m), 5.31–5.43(2H, m), 6.34(1H, d, J=6.6 Hz),6.77 (1H, m), 7.41, 7.55 and 7.58(each 1H, each d, each J=3.9 Hz).IR(CHCl₃): 3511, 3442, 3373, 3096, 1708, 1655, 1530, 1504, 1436, 1335,1152 cm⁻¹. [α]_(D) ^(26.5)+73.0±1.1°(c=1.002, MeOH) Anal.(C₂₄H₂₉NO₅S₃.0.3H₂O) Calcd.(%): C, 56.18; H, 5.81; N, 2.73; S, 18.75.Found(%): C, 56.26; H, 5.74; N, 2.65; S, 18.50.

Compound Number I-83

¹H-NMR(CDCl₃) δ: 1.17(1H, m), 1.24–1.36(2H, m), 1.37–1.82(6H, m),2.01–2.23 (5H, m), 2.36(2H, t, J=7.2 Hz), 2.51(1H, m), 3.83(1H, m),5.31–5.45 (2H, m, 7.17(1H, dd, J=3.9 and 5.4 Hz), 7.36(1H, d, J=7.8 Hz),7.47 (1H, dd, J=1.5 and 3.9 Hz), 7.66(1H, dd, J=1.5 and 5.4 Hz).IR(CHCl₃): 3514, 3404, 3121, 1709, 1657, 1544, 1488, 1425 cm⁻¹. [α]_(D)²⁵+73.2±2.2°(c=0.518, MeOH) Anal. (C₂₂H₂₆N₂O₃S₃.0.2H₂O) Calcd.(%): C,56.67; H, 5.71; N, 6.01; S, 20.63. Found(%): C, 56.55; H, 5.71; N, 6.03;S, 20.93.

Compound Number I-84

¹H-NMR(CDCl₃) δ: 1.07(1H, m), 1.20–1.32(2H, m), 1.43–1.48(2H, m),1.57–1.82(4H, m), 2.02(1H, d, J=3.3 Hz), 2.00–2.20(5H, m), 2.35(2H, t,J=7.2 Hz), 2.55(1H, m), 3.86(1H, m), 4.01(2H, s), 5.29–5.43(2H, m),6.17(1H, d, J=7.2 Hz), 7.15–7.31(7H, m), 7.67(2H, d, J=8.1 Hz).IR(CHCl₃): 3517, 3447, 2669, 1708, 1651, 1523, 1495 cm⁻¹. [α]_(D)²⁵+77.9±1.2°(c=1.016, MeOH) Anal. (C₂₈H₃₃NO₃) Calcd.(%): C, 77.93; H,7.71; N, 3.25. Found(%): C, 77.65; H, 7.93; N, 3.32.

Compound Number I-85

¹H-NMR(CDCl₃) δ: 1.08(1H, m), 1.21–1.31(2H, m), 1.44–1.49(2H, m),1.58–1.82(4H, m), 2.00–2.20(5H, m), 2.35(2H, t, J=7.2 Hz), 2.56(1H, m),3.87(1H, m), 4.19(2H, s), 5.30–5.43(2H, m), 6.19(1H, d, J=7.2 Hz),6.80(1H, m), 6.93(1H, dd, J=2.6 and 5.1 Hz), 7.16(1H, dd, J=1.5 and 5.1Hz), 7.30 and 8.69(each 2H, each d, each J=8.1 Hz). IR(CHCl₃): 3510,3446, 2664, 1708, 1651, 1523, 1496 cm⁻¹. [α]_(D) ²⁵+73.2±1.1°(c=1.009,MeOH) Anal. (C₂₆H₃₁NO₃S) Calcd.(%): C, 71.36; H, 7.14; N, 3.20; S, 7.33.Found(%): C, 71.48; H, 7.05; N, 3.29; S, 7.13.

Compound Number I-86

¹H-NMR(CDCl₃) δ: 1.07(1H, m), 1.19–1.31(2H, m), 1.43–1.48(2H, m),1.58–1.81(4H, m), 2.00–2.17(5H, m), 2.34(2H, t, J=7.2 Hz), 2.55(1H, m),3.87(1H, m), 3.98(2H, s), 5.30–5.43(2H, m), 6.19(1H, d, J=7.2 Hz),6.93–7.00(2H, m), 7.09–7.13(2H, m), 7.22 and 7.70(each 2H, each d, eachJ=8.4 Hz). IR(CHCl₃): 3516, 3447, 2664, 1709, 1651, 1612, 1522, 1509,1496, cm⁻¹. [α]_(D) ²⁵+71.6±1.1°(c=1.019, MeOH) Anal. (C₂₈H₃₂FNO₃)Calcd.(%): C, 74.81; H, 7.17; N, 3.12; F. 4.23. Found(%): C, 74.66; H,7.19; N, 3.13; F, 4.10.

Compound Number I-87

¹H-NMR(CDCl₃) δ: 1.08(1H, m), 1.20–1.31(2H, m), 1.44–1.49(2H, m),1.58–1.82(4H, m), 2.00–2.22(5H, m), 2.35(2H, t, J=7.2 Hz), 2.56(1H, m),3.87 (1H, m), 4.02(2H, s), 5.30–5.43(2H, m), 6.18(1H, d, J=7.2 Hz),6.88(1H, dd, J=1.5 and 4.8 Hz), 6.92(1H, m), 7.25–7.28(3H, m), 7.68(2H,d, J=8.1 Hz). IR(CHCl₃): 3516, 3446, 2668, 1709, 1651, 1612, 1523, 1496cm⁻¹. [α]_(D) ²⁵+72.7±1.1°(c=1.014, MeOH) Anal. (C₂₆H₃₁NO₃S.0.1H₂O)Calcd.(%): C, 71.07; H, 7.16; N, 3.18; S, 7.30. Found(%): C, 70.90; H,7.08; N, 3.21; S, 7.46.

Compound Number I-88

mp.103–105° C.; ¹H-NMR(CDCl₃) δ: 1.05(1H, m), 1.19–1.29(2H, m),1.42–1.47(2H, m), 1.58–1.81(4H, m), 2.00–2.15(5H, m), 2.35(2H, t, J=7.2Hz), 2.52(1H, m), 3.82(1H, m), 4.16(2H, s), 5.30–5.43(2H, m), 5.97(1H,d, J=7.5 Hz), 6.79(1H, dt, J=0.9 and 3.9 Hz), 6.96(1H, dd, J=1.5 and 4.8Hz), 7.05 (1H, m), 7.28(1H, dd, J=3.0 and 4.8 Hz), 7.37(1H, d, J=3.9Hz). IR(CHCl₃): 3516, 3445, 3427, 2670, 1708, 1642, 1544, 1507 cm⁻¹.[α]_(D) ²⁵+67.3±1.1°(c=1.002, MeOH) Anal. (C₂₄H₂₉NO₃S₂.0.3H₂O)Calcd.(%): C, 64.20; H, 6.64; N, 3.12; S, 14.28. Found(%): C, 64.29; H,6.49; N, 3.10; S, 14.11.

Compound Number I-89

¹H-NMR(CDCl₃) δ: 1.07(1H, m), 1.20–1.29(2H, m), 1.40–1.49(2H, m),1.56–1.89(4H, m), 2.00–2.25(6H, m), 2.32–2.38(2H, m), 2.51(1H, m), 3.80(1H, m), 5.04(2H, s), 5.27–5.41(2H, m), 5.90(1H, d, J=6.6 Hz), 6.38(1H,m), 6.63(1H, t, J=2.4 Hz), 7.14–7.17(2H, m), 7.29–7.35(4H, m).IR(CHCl₃): 3510, 3448, 2663, 1736, 1709, 1636, 1555, 1497 cm⁻¹. [α]_(D)²⁵+60.8±1.0°(c=1.003, MeOH) Anal. (C₂₆H₃₂N₂O₃.0.3H₂O) Calcd.(%): C,73.62; H, 7.70; N, 6.60. Found(%): C, 73.68; H, 7.62; N, 6.73.

Compound Number I-90

¹H-NMR(CDCl₃) δ: 1.06(1H, m), 1.20–1.29(2H, m), 1.40–1.48(2H, m),1.56–1.87(4H, m), 2.00–2.24(5H, m), 2.32–2.38(2H, m), 2.50(1H, m), 3.80(1H, m), 5.19(2H, s), 5.27–5.41(2H, m), 5.90(1H, d, J=7.5 Hz), 6.37(1H,dd, J=2.1 and 3.0 Hz), 6.67(1H, t, J=2.4 Hz), 6.95–6.98(2H, m), 7.27(1H,dd, J=1.8 and 4.5 Hz), 7.31(1H, dd, J=1.8 and 2.1 Hz). IR(CHCl₃): 3513,3448, 2661, 1709, 1637, 1555, 1497 cm⁻¹. [α]_(D) ²⁵+59.4±1.0°(c=1.011,MeOH) Anal. (C₂₄H₃₀N₂O₃S.0.2H₂O) Calcd.(%): C, 67.01; H, 7.12; N, 6.51;S, 7.45. Found(%): C, 67.07; H, 7.03; N, 6.62; S, 7.55.

Compound Number I-91

¹H-NMR(CDCl₃) δ: 1.06(1H, m), 1.23–1.26(2H, m), 1.39–1.48(2H, m),1.57–1.82(4H, m), 2.00–2.16(5H, m), 2.34(2H, t, J=7.2 Hz), 2.50(1H, m),3.82(1H, m), 5.03(2H, s), 5.27–5.42(2H, m), 5.98(1H, brs), 6.40(1H, m),6.91(1H, dd, J=1.2 and 4.8 Hz), 7.08(1H, brs), 7.28–7.31(2H, m).IR(CHCl₃): 3516, 3448, 3108, 2663, 1736, 1709, 1636, 1555, 1497 cm⁻¹.[α]_(D) ²⁵+59.8±1.0°(C=1.008, MeOH) Anal. (C₂₄H₃₀N₂O₃S.0.2H₂O)Calcd.(%): C, 67.01; H, 7.12; N, 6.51; S, 7.45. Found(%): C, 67.26; H,7.06; N, 6.61; S, 7.55.

Compound Number I-92

¹H-NMR(CDCl₃) δ: 1.08(1H, m), 1.18–1.28(2H, m), 1.38–1.43(2H, m),1.54–1.78(4H, m), 1.96–2.23(5H, m), 2.36(2H, dt, J=1.8 and 6.9 Hz), 2.52(1H, m) 3.77(1H, m), 5.30–5.45(2H, m), 6.07(1H, d, J=6.9 Hz), 6.58(1H,dd, J=1.5 and 3.3 Hz), 7.14(1H, dd, J=2.1 and 3.3 Hz), 7.51–7.57(2H, m),7.65 (1H, m), 7.77(1H, t, J=2.1 Hz), 7.88–7.92(2H, m). IR(CHCl₃): 3510,3444, 3144, 1732, 1708, 1651, 1570, 1509, 1382, 1176 cm⁻¹. [α]_(D)²⁴+55.9±0.9°(c=1.013, MeOH) Anal. (C₂₅H₃₀N₂O₅S.0.3H₂O) Calcd.(%): C,63.08; H, 6.48; N, 5.88; S, 6.74. Found(%): C, 63.24; H, 6.27; N, 6.03;S, 6.74.

Compound Number I-93

¹H-NMR(CDCl₃) δ: 1.06(1H, m), 1.18–1.29(2H, m), 1.39–1.47(2H, m),1.56–1.78 (4H, m), 1.98–2.18(5H, m), 2.35(2H, t, J=7.2 Hz), 2.52(1H, m),3.81(1H, m), 4.33(2H, s), 5.29–5.42(2H, m), 6.03(1H, d, J=7.5 Hz),6.84(1H, d, J=3.9 Hz), 6.90(1H, m), 6.95(1H, dd, J=3.6 and 5.1 Hz),7.19(1H, dd, J=1.2 and 5.1 Hz), 7.38(1H, d, J=3.9 Hz). IR(CHCl₃): 3510,3554, 3427, 1708, 1643, 1544, 1507 m⁻¹. [α]_(D) ²⁷+70.1±1°(c=1.010,MeOH) Anal. (C₂₄H₂₉NO₂₉NO₃S₂.0.1H₂O) Calcd.(%): C, 64.72; H, 6.61; N,3.14; S, 14.40. Found(%): C, 64.83; H, 6.60; N, 3.31; S, 14.46.

Compound Number I-94

¹H-NMR(CDCl₃) δ: 1.09(1H, m), 1.20–1.27(2H, m), 1.40–1.44(2H, m),1.56–1.78(4H, m), 2.00–2.19(5H, m), 2.36(2H, d, J=7.2 Hz), 2.51(1H, m),3.78 (1H, m), 5.30–5.44(2H, m), 6.13(1H, d, J=6.9 Hz), 6.59(1H, dd,J=1.5 and 3.3 Hz), 7.10(1H, dd, J=3.6 and 5.1 Hz), 7.16(1H, dd, J=2.1and 3.3 Hz), 7.69–7.76(3H, m). IR(CHCl₃): 3510, 3444, 3143, 1708, 1651,1571, 1508, 1387, 1179 cm⁻¹. [α]_(D) ²⁴+56.0±1.0°(c=1.005, MeOH) Anal.(C₂₃H₂₈N₂O₅S₂.0.2H₂O) Calcd.(%): C, 57.53; H, 5.96; N, 5.83; S, 13.35.Found(%): C, 57.54; H, 6.07; N, 5.93; S, 12.91.

Compound Number I-95

¹H-NMR(CDCl₃) δ: 1.16(1H, m), 1.26–1.37(2H, m), 1.40–1.81(6H, m),2.04–2.25(5H, m), 2.36(2H, t, J=7.2 Hz), 2.53(1H, m), 3.87(1H, m),5.32–5.46 (2H, m), 6.37(2H, t, J=2.1 Hz), 7.31(1H, d, J=7.5 Hz),7.33(2H, t, J=2.1 Hz), 7.82(1H, m). IR(CHCl₃): 3512, 3408, 3127, 1708,1658, 1540, 1525, 1493, 1341 m⁻¹. [α]_(D) ²⁵+88.2±1.3°(c=1.003, MeOH)Anal. (C₂₂H₂₇N₃O₃S.0.1H₂O) Calcd.(%): C, 63.62; H, 6.60; N, 10.12; S,7.72. Found(%): C, 63.72; H, 6.45; N, 9.99; S, 7.75.

Compound Number I-96

¹H-NMR(CDCl₃) δ: 1.07(1H, m), 1.18–1.30(2H, m), 1.39–1.48(2H, m),1.57–1.78(4H, m), 2.01–2.22(5H, m), 2.35(2H, t, J=7.2 Hz), 2.52(1H, m),3.80(1H, m), 5.30–5.43(2H, m), 6.11(1H, m), 6.98(1H, dd, J=3.6 and 5.4Hz), 7.24(1H, dd, J=1.2 and 3.6 Hz), 7.38(1H, dd, J=1.2 and 5.4 Hz),7.43 (1H, d, J=1.5 Hz), 7.85(1H, d, J=1.5 Hz). IR(CHCl₃): 3510, 3445,3108, 1708, 1650, 1535, 1498 m⁻¹. [α]_(D) ²⁵+70.7±1.1°(c=1.004, MeOH)Anal. (C₂₃H₂₇NO₃S₃.0.3H₂O) Calcd.(%): C, 59.15; H, 5.96; N, 3.00; S,20.60. Found(%): C, 59.06; H, 5.66; N, 3.07; S, 20.87.

Compound Number I-97

¹H-NMR(CDCl₃) δ: 1.20–2.52(16H, m), 2.61(1H, m), 3.72(1H, m), 5.34–5.55(2H, m), 6.66(1H, d, J=6.3 Hz), 71.2(1H, m), 7.71(1H, m), 7.75(1H, m),8.29(1H, m), 8.37(1H, brs). IR(CHCl₃): 3512, 3405, 3096, 1726, 1710,1653, 1542, 1505, 1402, 1329, 1152 m⁻¹. [α]_(D) ²⁵+65.4±1.1°(c=1.005,MeOH) Anal. (C₂₃H₂₇NO₅S₃.0.2H₂O) Calcd.(%): C, 55.55; H, 5.55; N, 2.82;S, 19.35. Found(%): C, 55.47; H, 5.54; N, 3.09; S, 19.21.

Compound Number I-98

mp.103–104° C.; ¹H-NMR(CDCl₃) δ: 1.09(1H, m), 1.23–1.31(2H, m),1.45–1.50(2H, m), 1.60–1.80(4H, m), 2.00–2.23(5H, m), 2.37(2H, t, J=7.2Hz), 2.55 (1H, m), 3.85(1H, m), 5.31–5.45(2H, m), 6.05(1H, d, J=7.5 Hz),6.98 and 7.04(each 1H, each d, each J=16.2 Hz), 6.97(1H, d, J=3.9 Hz),7.25–7.33 (3H, m), 7.41(1H, d, J=3.9 Hz). IR(CHCl₃): 3511, 3445, 3428,2665, 1708, 1641, 1538, 1519, 1499 cm⁻¹. [α]_(D) ²⁴+77.8±1.2°(c=1.007,MeOH) Anal. (C₂₅H₂₉NO₃S₂.0.25AcOEt) Calcd.(%): C, 65.38; H, 6.54; N,2.93; S, 13.43. Found(%): C, 65.64; H, 6.62; N, 2.95; S, 13.26.

Compound Number I-99

¹H-NMR(CDCl₃) δ: 1.05(1H, m), 1.20–1.30(2H, m), 1.41–1.46(2H, m),1.59–1.80(4H, m), 2.00–2.20(5H, m), 2.35(2H, t, J=7.2 Hz), 2.52(1H, m),3.80(1H, m), 5.30–5.43(2H, m), 5.94(1H, d, J=6.9 Hz), 6.57(2H, s),6.94(1H, d, J=3.9 Hz), 7.03(1H, dd, J=1.5 and 4.5 Hz), 7.29(1H, s),7.30(1H, m), 7.34 (1H, d, J=3.91 Hz). IR(CHCl₃): 3511, 3445, 3427, 2670,1708, 1642, 1536, 1518, 1500 cm⁻¹. [α]_(D) ²⁴+62.8±1.0°(c=1.003, MeOH)Anal. (C₂₅H₂₉NO₃S₂.0.2AcOEt) Calcd.(%): C, 65.48; H, 6.52; N, 2.96; S,13.55. Found(%): C, 65.36; H, 6.47; N, 2.13; S, 13.58.

Compound Number I-100

¹H-NMR(CDCl₃) δ: 1.06(1H, m), 1.17–1.32(2H, m), 1.38–1.50(2H, m),1.56–1.80 (4H, m), 1.98–2.20(5H, m), 2.35(2H, t, J=7.2 Hz), 2.44(3H, d,J=0.9 Hz), 2.52(1H, m), 3.80(1H, m), 5.30–5.43(2H, m), 5.99(1H, d, J=7.5Hz), 5.99(1H, d, J=7.5. Hz), 6.70(1H, m), 7.03(1H, d, J=3.9 Hz),7.10(1H, d, J=1.5 Hz), 7.36(1H, d, J=3.9 Hz). IR(CHCl₃): 3510, 3445,3426, 2671, 1708, 1644, 1530, 1499, 1420, 1318 cm⁻¹. [α]_(D)²⁵+69.1±1.1°(c=1.018, MeOH) Anal. (C₂₄H₂₉NO₃S₃) Calcd.(%): C, 60.60; H,6.14; N, 2.94; S, 20.22. Found(%): C, 60.49; H, 6.26; N, 2.98; S, 20.25.

Compound Number I-101

¹H-NMR(CDCl₃) δ: 1.10(1H, m), 1.18–1.32(2H, m), 1.38–1.50(2H, m),1.54–1.77 (4H, m), 2.00–2.20(5H, m), 2.36(2H, t, J=7.2 Hz), 2.47(3H, d,J=0.9 Hz), 2.53(1H, m), 3.81(1H, m), 5.31–5.44(2H, m), 6.30(1H, d, J=7.2Hz), 7.03(1H, m), 7.42 and 7.59(each 1H, each d, each J=3.9 Hz),7.90(1H, d, J=1.5 Hz). IR(CHCl₃): 3517, 3441, 3370, 3115, 2671, 1708,1655, 1530, 1504, 1442, 1328, 1156, 1142 cm⁻¹. [α]_(D)²⁴+71.6±1.1°(c=1.018, MeOH) Anal. (C₂₄H₂₉NO₅S₃.0.2H₂O) Calcd.(%): C,56.38; H, 5.80; N, 2.74; S, 18.81. Found(%): C, 56.28; H, 5.74; N, 2.79;S, 18.92.

Compound Number I-102

¹H-NMR(CDCl₃) δ: 1.09(1H, m), 1.21–1.28(2H, m), 1.42–1.47(2H, m),1.57–1.74(4H, m), 2.00–2.18(5H, m), 2.35(2H, t, J=7.2 Hz), 2.53(1H, m),3.82 (1H, m), 5.30–5.43(2H, m), 6.15(1H, d, J=7.5 Hz), 6.51 and6.68(each 1H, each d, J=11.7 Hz), 6.98(1H, dd, J=3.6 and 5.1 Hz),7.06(1H, dd, J=0.9 and 3.9 Hz), 7.13(1H, dt, J=0.9 and 3.6 Hz), 7.25(1H,dd, J=0.9 and 5.1 Hz), 7.41(1H, d, J=3.9 Hz). IR(CHCl₃): 3510, 3445,3427, 2665, 1708, 1643, 1535, 1501 cm⁻¹. [α]_(D) ²⁴+68.6±1.1°(c=1.006,MeOH) Anal. (C₂₅H₂₉NO₃S₂.0.2H₂O) Calcd.(%): C, 65.45; H, 6.45; N, 3.05;S, 13.98. Found(%): C, 65.44; H, 6.37; N, 3.28; S, 13.82.

Compound Number I-103

mp.107–108° C.; ¹H-NMR(CDCl₃) δ: 1.09(1H, m), 1.26–1.32(2H, m),1.45–1.50 (2H, m), 1.60–1.81(4H, m), 2.01–2.23(5H, m), 2.37(2H, t, J=7.2Hz), 2.55 (1H, m, 3.84(1H, m), 5.31–5.45(2H, m), 6.03(1H, d, J=7.5 Hz),6.97 and 7.14(each 1H, each d, J=15.9 Hz), 6.97(1H, d, J=3.9 Hz),7.01(1H, dd, J=3.6 and 5.4 Hz), 7.08(1H, d, J=3.6 Hz), 7.23(1H, d, J=5.4Hz), 7.40(1H, d, J=3.9 Hz). IR(CHCl₃): 3517, 3445, 3428, 2670, 1708,1641, 1536, 1518, 1500 cm⁻¹. [α]_(D) ²⁴+85.0±1.2°(c=1.009, MeOH) Anal.(C₂₅H₂₉NO₃S₂.0.15AcOEt) Calcd.(%): C, 65.58; H, 6.49; N, 2.99; S, 13.68.Found(%): C, 65.88; H, 6.74; N, 2.98; S, 13.35.

Compound Number I-104

¹H-NMR(CDCl₃) δ: 1.07(1H, m), 1.19–1.30(2H, m), 1.42–1.50(2H, m),1.57–1.79(4H, m), 2.01–2.24(5H, m), 2.36(2H, t, J=7.2 Hz), 2.53(1H, m),3.82 (1H, m), 4.10(sH, s), 5.31–5.44(2H, m), 6.03(1H, d, J=7.2 Hz),6.70(1H, d, J=3.6 Hz), 6.95(1H, dd, J=3.6 and 5.4 Hz), 7.03(1H, dd,J=1.5 and 3.6 Hz), 7.30(1H, d, J=3.6 Hz), 7.36(1H, dd, J=1.5 and 5.4Hz). IR(CHCl₃): 3518, 3445, 3427, 1708, 1644, 1542, 1507 cm⁻¹. [α]_(D)^(24.5)+65.0±1.0°(c=1.008, MeOH) Anal. (C₂₄H₂₉NO₃S₃.0.4H₂O) Calcd.(%):C, 59.69; H, 6.22; N, 2.90; S, 19.92. Found(%): C, 59.40; H, 5.98; N,2.95; S, 20.06.

Compound Number I-105

¹H-NMR(CDCl₃) δ: 1.11(1H, m), 1.21–1.31(2H, m), 1.42–1.49(2H, m),1.58–1.76(4H, m), 2.01–2.21(5H, m), 2.36(2H, t, J=7.2 Hz), 2.53(1H, m),3.81 (1H, m), 4.60(sH, s), 5.32–5.45(2H, m), 6.18(1H, d, J=7.2 Hz),6.91(1H, d, J=3.9 Hz), 7.12(1H, dd, J=3.9 and 5.1 Hz), 7.40(1H, d, J=3.9Hz), 7.52 (1H, dd, J=1.2 and 3.9 Hz), 7.72(1H, dd, J=1.2 and 5.1 Hz).IR(CHCl₃): 3517, 3444, 3425, 3097, 1708, 1648, 1524, 1508, 1402, 1328,1147 cm⁻¹. [α]_(D) ^(24.5)+61.5±1.0°(c=1.008, MeOH) Anal.(C₂₄H₂₉NO₅S₂.0.4H₂O) Calcd.(%): C, 55.98; H, 5.83; N, 2.72; S, 18.68.Found(%): C, 55.77; H, 5.71; N, 2.84; S, 18.73.

Compound Number I-106

¹H-NMR(CDCl₃) δ: 1.07(1H, m), 1.19–1.31(2H, m), 1.41–1.49(2H, m),1.57–1.78(4H, m), 2.00–2.21(5H, m), 2.36(2H, t, J=7.2 Hz), 2.53(1H, m),3.81 (1H, m), 4.23(sH, s), 5.31–5.44(2H, m), 6.00(1H, d, J=7.2 Hz),6.82(1H, m), 6.88(1H, dd, J=3.6 and 5.1 Hz), 6.92(1H, d, J=3.6 Hz),7.21(1H, dd, J=1.2 and 5.1 Hz), 7.33(1H, d, J=3.6 Hz). IR(CHCl₃): 3514,3444, 3427, 2665, 1709, 1645, 1529, 1498, 1421, 1317 cm⁻¹. [α]_(D)²⁴+67.1±1.1°(c=1.006, MeOH) Anal. (C₂₄H₂₉NO₃S₃.0.1H₂O) Calcd.(%): C,60.37; H, 6.16; N, 2.90; S, 20.15. Found(%): C, 60.46; H, 6.14; N, 2.96;S, 20.02.

Compound Number I-107

¹H-NMR(CDCl₃) δ: 1.09–1.32(3H, m), 1.38–1.48(2H, m), 1.53–1.79(4H, m),1.96–2.20(5H, m), 2.34(2H, t, J=7.2 Hz), 2.54(4H, d and m, J=0.6 Hz),3.79 (1H, m), 5.30–5.45(2H, m), 6.48 and 6.51(total 1H, each d, J=7.8and 7.5 Hz), 7.12 (1H, dd, J=3.9 and 5.1 Hz), 7.42 and 7.43(total 1H,each d, each J=3.9 Hz), 7.52 and 7.53(total 1H, each d, each J=3.9 Hz),7.58(1H, m), 7.69 (1H, dd, J=1.2 and 5.1 Hz). IR(CHCl₃): 3509, 3443,3425, 3092, 2666, 1708, 1650, 1532, 1503, 1403, 1322 cm⁻¹. [α]_(D)²³+70.4±1.1°(c=1.007, MeOH) Anal. (C₂₃H₂₇NO₄S₃.0.4H₂O) Calcd.(%): C,56.97; H, 5.78; N, 2.89; S, 19.84. Found(%): C, 57.03; H, 5.67; N, 3.19;S, 19.73.

Compound Number I-108

¹H-NMR(CDCl₃) δ: 1.09–1.32(3H, m), 1.39–1.50(2H, m), 1.54–1.77(4H,m),1.97–2.20(5H ,m), 2.35(2H, t, J=7.2 Hz), 2.52 and 2.53(total 3H, eachs), 2.54(1H, m), 3.79(1H, m), 5.31–5.45(2H, m), 6.43 and 6.47(total 1H,each d, J=7.5 and 6.6 Hz), 6.76(1H, m), 7.39(1H, t-like), 7.40(1H, dd,J=2.1 and 3.6 Hz), 7.52(1H, dd, J=2.1 and 4.2 Hz). IR(CHCl₃): 3510,3443, 3425, 3092, 1708, 1650, 1531, 1503, 1437, 1237 cm⁻¹. [α]_(D)²³68.6±1.1°(c=1.011, MeOH) Anal. (C₂₄H₂₉NO₄S₃.0.2H₂O) Calcd.(%): C,58.20; H, 5.98; N, 2.83; S, 19.42. Found(%): C, 58.18; H, 5.67; N, 2.90;S, 19.11.

Compound Number I-109

¹H-NMR(CDCl₃) δ: 1.13(1H, m), 1.21–1.34(2H, m), 1.45–1.52(2H, m),1.59–1.78(4H, m), 2.03–2.23(5H, m), 2.37(2H, t, J=7.2 Hz), 2.58(1H, m),3.86(1H, m), 5.32–5.46(2H, m), 6.28(1H, d, J=6.6 Hz), 7.20(1H, dd, J=3.9and 5.1 Hz), 7.59(1H, d, J=3.9 Hz), 7.75(1H, dd, J=1.2 and 5.1 Hz),7.81(1H, d, J=3.9 Hz), 7.92(1H, dd, J=1.2 and 3.9 Hz). IR(CHCl₃): 3518,3442, 3425, 3109, 1709, 1651, 1622, 1529, 1508, 1442, 1414, 1356, 1286,1267 cm⁻¹. [α]_(D) ²³+89.2±1.3°(c=1.002, MeOH) Anal.(C₂₄H₂₇NO₄S₂.0.2H₂O) Calcd.(%): C, 62.50; H, 5.99; N, 3.04; S, 13.90.Found(%): C, 62.63; H, 6.07; N, 2.97; S, 13.60.

Compound Number I-110

¹H-NMR(CDCl₃) δ: 1.12(1H, m), 1.22–1.33(2H, m), 1.44–1.52(2H, m),1.59–1.79 (4H, m), 2.03–2.24(5H, m), 2.37(2H, t, J=7.2 Hz), 2.57(1H, m),3.87(1H, m), 4.14(3H, s), 5.32–5.47(2H, m), 6.14(1H, d, J=7.5 Hz),7.08(1H, dd, J=3.9 and 5.4 Hz), 7.27(1H, dd, J=1.2 and 3.9 Hz), 7.39(1H,dd, J=1.2 and 5.4 Hz), 7.41(1H, d, J=3.9 Hz), 7.49(1H, d, J=3.9 Hz).IR(CHCl₃): 3516, 3444, 3425, 2665, 1709, 1649, 1529, 1498, 1049 cm⁻¹.[α]_(D) ²⁴+73.3±1.1°(c=1.003, MeOH) Anal. (C₂₅H₃₀N₂O₄S₂.0.6H₂O)Calcd.(%): C, 60.36; H, 6.32; N, 5.63; S, 12.89. Found(%): C, 60.30; H,6.14; N, 5.84; S, 12.95.

Compound Number I-111

¹H-NMR(CDCl₃) δ: 1.08(1H, m), 1.19–1.30(2H, m), 1.40–1.50(2H, m),1.55–1.82(4H, m), 1.98–2.21(5H ,m), 2.36(2H, t, J=7.2 Hz), 2.53(1H, m),3.83(1H, m), 5.30–5.44(2H, m), 5.96(1H, d, J=7.5 Hz), 6.43(1H, br), 6.52(1H, d, J=3.9 Hz), 6.90(1H, m), 7.08–7.11(2H, m), 7.26–7.32(3H, m).IR(CHCl₃): 3514, 3444, 3419, 1739, 1709, 1633, 1601, 1500, 1456 cm⁻¹.[α]_(D) ²²+86.6±1.3°(c=1.005, MeOH) Anal. (C₂₅H₃₀N₂O₃S.0.1H₂O)Calcd.(%): C, 68.18; H, 6.91; N, 6.36; S, 7.28. Found(%): C, 68.11; H,6.95; N, 6.43; S, 7.31.

Compound Number I-112

¹H-NMR(CDCl₃) δ: 1.05(1H, m), 1.18–1.30(2H, m), 1.39–1.48(2H, m),1.54–1.83(4H, m), 1.98–2.21(5H ,m), 2.35(2H, t, J=7.2 Hz), 2.51(1H, m),3.38 (3H, s), 3.80(1H, m), 5.29–5.42(2H, m), 5.82(1H, d, J=6.0 Hz),6.15(1H, d, J=4.2 Hz), 7.11–7.39(6H, m). IR(CHCl₃): 3514, 3446, 3425,1741, 1709, 1628, 1597, 1477, 1415 cm⁻¹. [α]_(D) ²²+83.2±1.2°(c=1.001,MeOH) Anal. (C₂₆H₃₂N₂O₃S) Calcd.(%): C, 69.00; H, 7.13; N, 6.19; S,7.08. Found(%): C, 68.74; H, 7.08; N, 6.15; S, 7.01.

Compound Number I-113

¹H-NMR(CDCl₃) δ: 1.07(1H, m), 1.18–1.31(2H, m), 1.40–1.49(2H, m),1.55–1.75(4H, m), 1.99–2.16(5H, m), 2.31(3H, s), 2.35(2H, t, J=7.2 Hz),2.52 (1H, m), 3.82(1H, m), 5.31–5.43(2H, m), 6.06(1H, d, J=7.5 Hz),7.03–7.20 (5H, m), 7.44(1H, d, J=3.9 Hz). IR(CHCl₃): 3516, 3444, 3425,2671, 1709, 1647, 1529, 1498, 1421, 1317 cm⁻¹. [α]_(D)²³+70.2±1.1°(c=1.001, MeOH) Anal. (C₂₆H₃₁NO₃S₂) Calcd.(%): C, 66.49; H,6.65; N, 2.98; S, 13.65. Found(%): C, 66.34; H, 6.74; N, 2.94; S, 13.78.

Compound Number I-114

mp.114–116° C.; ¹H-NMR(CDCl₃) δ: 1.09(1H, m), 1.18–1.32(2H, m),1.37–1.47 (2H, m), 1.55–1.75(4H, m), 2.00–2.18(5H, m), 2.35(2H, t, J=7.2Hz), 2.42 (3H, s), 2.52(1H, m), 3.80(1H, m), 5.30–5.43(2H, m), 6.23(1H,d, J=7.5 Hz), 7.41(3H, m), 7.59(1H, d, J=3.9 Hz), 7.78(2H, m).IR(CHCl₃): 3514, 3442, 3371, 2669, 1707, 1655, 1529, 1504, 1329, 1151cm⁻¹. [α]_(D) ²³+72.4±1.1°(c=1.004, MeOH) Anal. (C₂₆H₃₁NO₅S₂) Calcd.(%):C, 62.25; H, 6.23; N, 2.79; S, 12.78. Found(%): C, 61.83; H, 6.39; N,2.73; S, 12.78.

Compound Number I-115

¹H-NMR(CDCl₃) δ: 1.07(1H, m), 1.18–1.31(2H, m), 1.40–1.50(2H, m),1.56–1.78(4H, m), 1.99–2.20(5H, m), 2.35(2H, t, J=7.2 Hz), 2.53(1H, m),3.77(3H, s), 3.82(1H, m), 5.31–5.43(2H, m), 6.06(1H, d, J=7.2 Hz),6.74–6.89(3H, m), 7.16–7.23(2H, m), 7.45(1H, d, J=3.9 Hz). IR(CHCl₃):3516, 3444, 3425, 2665, 1709, 1647, 1591, 1529, 1498, 1477, 1423 cm⁻¹.[α]_(D) ²³+68.7±1.1°(c=1.014, MeOH) Anal. (C₂₆H₃₁NO₄S₂) Calcd.(%): C,64.30; H, 6.43; N, 2.88; S, 13.20. Found(%): C, 64.04; H, 6.56; N, 2.87;S, 13.43.

Compound Number I-116

mp.67–70° C.; ¹H-NMR(CDCl₃) δ: 1.09(1H, m), 1.17–1.32(2H, m), 1.39–1.47(2H, m), 1.55–1.75(4H, m), 2.00–2.20(5H, m), 2.35(2H, t, J=7.2 Hz), 2.52(1H, m), 3.80(1H, m), 3.86(3H, s), 5.30–5.43(2H, m), 6.26(1H, d, J=7.2Hz), 7.12 (1H, m), 7.40–7.47(2H, m), 7.55(1H, m), 7.59(1H, d, J=3.9 Hz).IR (CHCl₃): 3514, 3442, 3373, 1707, 1655, 1599, 1529, 1504, 1481, 1327,1151 cm⁻¹. [α]_(D) ²³+70.0±1.1°(c=1.008, MeOH) Anal.(C₂₆H₃₁NO₆S₂.0.7H₂O) Calcd.(%): C, 58.89; H, 6.16; N, 2.64; S, 12.09.Found(%): C, 58.87; H, 6.15; N, 2.74; S, 12.10.

Compound Number I-117

¹H-NMR(CDCl₃) δ: 1.10–1.32(3H, m), 1.37–1.46(2H, m), 1.55–1.73(4H, m),1.94–2.18(5H, m), 2.34(2H, t, J=7.2 Hz), 2.55(1H, m), 3.78(1H, m),5.29–5.45(2H, m), 6.56(1H, d, J=6.6 Hz), 7.09(1H, m), 7.37(1H, t, J=8.1Hz), 7.45 (1H, d, J=3.9 Hz), 7.47–7.53(2H, m), 7.55(1H, (d, J=3.9 Hz).IR(KBr): 3365, 3095, 1707, 1628, 1543, 1448, 1306, 1147 cm⁻¹. [α]_(D)²³+70.8±1.1°(c=1.003, MeOH) Anal. (C₂₅H₂₉NO₆S₂.0.3H₂O) Calcd.(%): C,58.99; H, 5.86; N, 2.75; S, 12.60. Found(%): C, 58.85; H, 5.85; N, 2.67;S, 12.77.

Compound Number I-118

mp.133–134° C.; ¹H-NMR(CDCl₃) δ: 1.08(1H, m), 1.18–1.32(2H, m),1.40–1.49 (2H, m), 1.55–1.78(4H, m), 1.96–2.24(5H, m), 2.34(2H, t, J=7.2Hz), 2.52(1H, m), 3.81(1H, m), 5.31–5.46(2H, m), 6.14(1H, d, J=6.6 Hz),6.71 (2H, m), 6.86(1H, m), 7.14(2H, m), 7.42(1H, d, J=3.9 Hz).IR(Nujol): 3336, 3091, 2656, 1703, 1603, 1581, 1545 cm⁻¹. [α]_(D)²³+73.2±1.1°(c=1.007, MeOH) Anal. (C₂₅H₂₉NO₄S₂) Calcd.(%): C, 63.67; H,6.20; N, 2.97; S, 13.60. Found(%): C, 63.78; H, 6.17; N, 3.10; S, 13.73.

Compound Number I-119

¹H-NMR(CDCl₃) δ: 1.05(1H, m), 1.17–1.30(2H, m), 1.38–1.48(2H, m),1.54–1.80 (4H, m), 1.98–2.20(5H, m), 2.34(2H, t, J=7.2 Hz), 2.51(1H, m),3.79 (3H, s), 3.81(1H, m), 4.10(2H, s), 5.29–5.42(2H, m), 5.97(1H, d,J=7.5 Hz), 6.77–6.84(4H, m), 7.23(2H, m), 7.37(1H, d, J=3.9 Hz). IR(CHCl₃): 3514, 3446, 3427, 1741, 1709, 1641, 1543, 1506, 1456 cm⁻¹.[α]_(D) ²²+64.3±1.0°(c=1.005, MeOH) Anal. (C₂₇H₃₃NO₄S.0.1H₂O) Calcd.(%):C, 69.08; H, 7.13; N, 2.98; S, 6.83. Found(%): C, 69.03; H, 7.25; N,3.06; S, 7.00.

Compound Number I-120

¹H-NMR(CDCl₃) δ: 1.07(1H, m), 1.16–1.28(2H, m), 1.36–1.46(2H, m),1.52–1.78 (4H, m), 1.96–2.17(5H, m), 2.32(2H, t, J=7.2 Hz), 2.50(1H, m),3.80(1H, m), 4.02(2H, s), 5.28–5.42(2H, m), 6.16(1H, d, J=7.5 Hz),6.72–6.77(4H, m), 1H, m), 7.36(1H, d, J=3.9 Hz). IR(CHCl₃): 3595, 3423,3207, 1707, 1635, 1599, 1545, 1508, 1456 cm⁻¹. [α]_(D)²³+66.8±1.1°(c=1.009, MeOH) Anal. (C₂₆H₃₁NO₄S.0.4H₂O) Calcd.(%): C,67.77; H, 6.96; N, 3.04; S, 6.96. Found(%): C, 67.83; H, 6.92; N, 3.18;S, 7.14.

Compound Number I-121

¹H-NMR(CDCl₃) δ: 1.06(1H, m), 1.8–1.31(2H, m), 1.40–1.48(2H, m),1.55–1.82(4H, m), 1.98–2.22(5H, m), 2.29(3H, s), 2.35(2H, t, J=7.2 Hz),2.52 (1H, m), 3.80(1H, m), 4.14(2H, s), 5.29–5.43(2H, m), 5.97(1H, d,J=7.5 Hz), 6.78 (1H, m), 6.94–7.00(2H, m), 7.10(1H, m), 7.33(1H, m),7.36(1H, d, J=3.9 Hz). IR(CHCl₃): 3514, 3446, 3427, 2669, 1763, 1745,1709, 1643, 1545, 1506, 1371 cm⁻¹. [α]_(D) ²³+61.3±1.0°(c=1.019, MeOH)Anal. (C₂₈H₃₃NO₅S.0.1H₂O) Calcd.(%): C, 67.61; H, 6.73; N, 2.82; S,6.45. Found(%): C, 67.52; H, 6.77; N, 2.99; S, 6.48.

Compound Number I-122

¹H-NMR(CDCl₃) δ: 1.06(1H, m), 1.18–1.30(2H, m), 1.40–1.48(2H, m),1.56–1.76(4H, m), 1.99–2.17(5H, m), 2.35(2H, t, J=7.2 Hz), 2.52(1H, m),3.81(1H, m), 4.25(2H, s), 5.30–5.43(2H, m), 6.00(1H, d, J=7.5 Hz),6.81(1H, d, J=3.9 Hz), 7.20–7.36(6H, m). IR(CHCl₃): 3516, 3446, 3427,2667, 1709, 1643, 1543, 1506 cm¹. [α]_(D) ²³+65.0±1.0°(c=1.008, MeOH)Anal. (C₂₆H₃₁NO₃S₂.0.1H₂O) Calcd.(%): C, 66.24; H, 6.67; N, 2.97; S,13.60. Found(%): C, 66.14; H, 6.63; N, 3.05; S, 13.49.

Compound Number I-123

¹H-NMR(CDCl₃) δ: 1.08(1H, m), 1.20–1.32(2H, m), 1.40–1.50 (2H, m),1.56–1.80 (4H, m), 2.00–2.20(5H, m), 2.36(2H, t, J=7.2 Hz), 2.54 (1H,m), 3.84 (1H, m), 5.20(2H, s), 5.31–5.44(2H, m), 6.06(1H, d, J=7.5 Hz),6.94–7.05 (4H, m), 7.27–7.33(2H, m), 7.42(1H, d, J=3.9 Hz). IR(CHCl₃):3516, 3444, 3427, 2669, 1709, 1645, 1599, 1545, 1508, 1497 cm⁻¹. [α]_(D)²⁴+65.4±1.1°(c=1.003, MeOH) Anal. (C₂₆H₃₁NO₄S.0.2H₂O) Calcd.(%): C,68.30; H, 6.92; N, 3.06; S, 7.01. Found(%): C, 68.32; H, 6.83; N, 3.08;S, 6.99.

Compound Number I-124

¹H-NMR(CDCl₃) δ: 1.06(1H, m), 1.18–1.32(2H, m), 1.40–1.50(2H, m),1.55–1.80(4H, m), 2.00–2.20(5H, m), 2.35(2H, t, J=7.2 Hz), 2.52(1H, m),3.81(1H, m), 4.51(2H, d, J=0.9 Hz), 5.30–5.43(2H, m), 6.01(1H, d, J=7.5Hz), 6.65–6.97(3H, m), 6.96(1H, d, J=3.9 Hz), 7.16–7.21(1H, m), 7.41(1H,d, J=3.9 Hz). IR(CHCl₃): 3516, 3444, 3427, 1709, 1643, 1603, 1545, 1504,1309, 1260 cm⁻¹. [α]_(D) ²²+65.7±1.0°(c=1.014, MeOH) Anal.(C₂₆H₃₂N₂O₃S.0.2H₂O) Calcd.(%): C, 68.45; H, 7.16; N, 6.14; S, 7.03.Found(%): C, 68.43; H, 7.18; N, 6.27; S, 6.94.

Compound Number I-125

¹H-NMR(CDCl₃) δ: 1.05(1H, m), 1.18–1.27(2H, m), 1.40–1.45(2H, m),1.56–1.77(4H, m), 2.00–2.13(5H, m), 2.28(3H, s), 2.34(2H, t, J=7.5 Hz),2.51(1H, m), 3.80(1H, m), 4.12(2H, s), 5.29–5.41(2H, m), 5.98(1H, d,J=7.2 Hz), 6.69(1H, d, J=3.6 Hz), 7.18(4H, s), 7.36(1H, d, J=3.6 Hz). IR(CHCl₃): 3518, 3446, 3426, 1741, 1709, 1641, 1543, 1506, 1458 cm⁻¹.[α]_(D) ^(22.5)+66.8±1.1°(c=1.003, MeOH) Anal. (C₂₇H₃₃NO₃S.H₂O)Calcd.(%): C, 69.05; H, 7.51; N, 2.98; S, 6.83. Found(%): C, 69.07; H,7.11; N, 3.23; S, 7.04.

Compound Number I-126

¹H-NMR(CDCl₃) δ: 1.04(1H, m), 1.17–1.28(2H, m), 1.41–1.46(2H, m),1.55–1.77(4H, m), 2.00–2.20(5H, m), 2.34(2H, t, J=7.2 Hz), 2.51(1H, m),3.80(1H, m), 4.12(2H, s), 5.29–5.41(2H, m), 5.91(1H, d, J=7.2 Hz),6.77(1H, d, J=3.3 Hz), 6.86–6.90(2H, m), 7.15(1H, dd, J=1.8 and 7.5 Hz),7.20–7.26 (1H, m), 7.34(1H, d, J=3.6 Hz). IR(CHCl₃): 3519, 3446, 3427,2669, 1741, 1709, 1641, 1543, 1504, 1458, 1248 cm⁻¹. [α]_(D)^(22.5)+64.2±1.0°(c=1.005, MeOH) Anal. (C₂₇H₃₃NO₄S.0.1H₂O) Calcd.(%): C,69.08; H, 7.13; N, 2.98; S, 6.83. Found(%): C, 68.97; H, 6.90; N, 3.09;S, 6.77.

Compound Number I-127

¹H-NMR(CDCl₃) δ: 1.04(1H, m), 1.18 (3H, t, J=7.7 Hz), 1.15–1.29 (2H, m),1.41–1.46 (2H, m), 1.56–1.80 (4H, m), 2.00–2.15 (5H, m), 2.35 (2H, t,J=7.2 Hz), 2.51 (1H, s), 2.64 (2H, q, J=7.7 Hz), 3.80 (1H, m), 4.16 (2H,s), 5.29–5.41 (2H, m), 5.91 (1H, d, J=7.5 Hz), 6.69 (1H, d, J=3.6 Hz),7.16–7.25 (4H, m), 7.35 (1H, d, J=3.6 Hz). IR (CHCl₃): 3516, 3447, 3427,2669, 1709, 1641, 1543, 1506, 1456 cm⁻¹. [α]_(D) ²¹+65.8±1.1°(c=1.011,MeOH). Anal. (C₂₈H₃₅NO₃S.0.2H₂O) Calcd.(%): C, 71.67; H, 7.60; N, 2.98;S, 6.83. Found(%): C, 71.83; H, 7.49; N, 3.12; S, 6.89.

Compound Number I-128

¹H-NMR(CDCl₃) δ: 1.04 (1H, m), 1.18–1.29 (2H, m), 1.41–1.46 (2H, m),1.56–1.80 (4H, m), 2.00–2.20 (5H, m), 2.24 and 2.31 (each 3H, each s),2.35 (2H, t, J=7.4 Hz), 2.51 (1H, s), 3.80 (1H, m), 4.19 (2H, s),5.29–5.41 (2H, m), 5.91 (1H, d, J=7.2 Hz), 6.70 (1H, d, J=3.6 Hz), 6.99(1H, d, J=7.5 Hz), 7.00 (1H, s), 7.07 (1H, d, J=7.5 Hz), 7.35 (1H, d,J=3.6 Hz). IR (CHCl₃): 3514, 3446, 3426, 1741, 1709, 1641, 1543, 1506,1456 cm⁻¹. [α]_(D) ²¹+65.2±1.0°(c=1.014, MeOH) Anal. (C₂₈H₃₅NO₃S.0.2H₂O)Calcd.(%): C, 71.67; H, 7.60; N, 2.98; S, 6.83. Found(%): C, 71.53; H,7.49; N, 3.31; S, 6.90.

Compound Number I-129

¹H-NMR(CDCl₃) δ: 1.05(1H, m), 1.18–1.29(2H, m), 1.42–1.47(2H, m),1.56–1.78(4H, m), 2.00–2.20(5H, m), 2.35(2H, t, J=7.5 Hz), 2.43(3H, s),2.52 (1H, s),3.81(1H, m), 4.24(2H, s), 5.30–5.42(2H, m), 5.97(1H, d,J=7.5 Hz), 6.57(1H, m), 6.67(1H, d, J=3.3 Hz), 6.83(1H, d, J=3.9 Hz),7.37 (1H, d, J=3.9 Hz). IR(CHCl₃): 3514, 3446, 3427, 1709, 1643, 1545,1506, 1456 cm⁻¹. [α]_(D) ²²+67.1±1.1°(c=1.002, MeOH) Anal. (C₂₅H₃₁NO₃S₂)Calcd.(%): C, 65.61; H, 6.83; N, 3.06; S, 14.01. Found(%): C, 65.42; H,6.76; N, 3.20; S, 13.73.

Compound Number I-130

¹H-NMR(CDCl₃) δ: 1.04(1H, m), 1.18–1.28(2H, m), 1.41–1.45(2H, m),1.55–1.78 (4H, m), 1.99–2.16(5H, m), 2.34(2H, t, J=7.2 Hz), 2.38(3H, s),2.51 (1H, m), 3.80(1H, m), 4.09(2H, s), 5.29–5.41(2H, m), 5.96(1H, d,J=6.9 Hz), 6.76(1H, d, J=3.6 Hz), 7.12(4H, s), 7.37(1H, d, J=3.6 Hz). IR(CHCl₃): 3510, 3446, 3427, 1741, 1709, 1641, 1543, 1508, 1458 cm⁻¹.[α]_(D) ²²+67.0±1.1°(c=1.014, MeOH) Anal. (C₂₇H₃₃NO₃S) Calcd.(%): C,71.81; H, 7.36; N, 3.10; S, 7.10. Found(%): C, 71.53; H, 7.24; N, 3.21;S, 7.36.

Compound Number I-131

¹H-NMR(CDCl₃) δ: 1.04(1H, m), 1.18–1.28(2H, m), 1.41–1.46(2H, m),1.56–1.78(4H, m), 1.99–2.19(5H, m), 2.33(3H, s), 2.34(2H, t, J=7.5 Hz),2.51 (1H, m), 3.81(1H, m), 4.09(2H, s), 5.29–5.42(2H, m), 5.96(1H, d,J=7.2 Hz), 6.77 (1H, d, J=3.6 Hz), 7.02–7.07(3H, m), 7.21(1H, m),7.37(1H, d, J=3.6 Hz). IR (CHCl₃): 3516, 3446, 3427, 1741, 1709, 1641,1543, 1506, 1458 cm⁻¹. [α]_(D) ²³+66.1±1.1°(c=1.006, MeOH) Anal.(C₂₇H₃₃NO₃S.0.2H₂O) Calcd.(%): C, 71.24; H, 7.40; N, 3.08; S, 7.04.Found(%): C, 71.26; H, 7.20; N, 3.19; S, 7.12.

Compound Number I-132

¹H-NMR(CDCl₃) δ: 1.06(1H, m), 1.19–1.30(2H, m), 1.41–1.49(2H, m),1.57–1.78(4H, m), 2.00–2.21(5H, m), 2.30(3H, s), 2.35(2H, t, J=7.2 Hz),2.52(1H, m), 3.81(1H, m), 4.25(2H, s), 5.30–5.43(2H, m), 6.01(1H, d,J=6.9 Hz), 6.82(1H, d, J=3.9 Hz), 7.02(1H, m), 7.10–7.19(3H, m),7.31(1H, d, J=3.9 Hz). IR(CHCl₃): 3516, 3446, 3427, 2671, 1739, 1709,1643, 1543, 1506, 1475, 1456 cm⁻¹. [α]_(D) ²³+63.2±1.0°(c=1.007, MeOH)Anal. (C₂₇H₃₃NO₃S₂.0.2H₂O) Calcd.(%): C, 66,55; H, 6.91; N, 2.87; S,13.16. Found(%): C, 66.44; H, 6.87; N, 2.99; S, 13.11.

Compound Number I-133

¹H-NMR(CDCl₃) δ: 1.07(1H, m), 1.20–1.30(2H, m), 1.45–1.51(2H, m),1.56–1.82(4H, m), 2.00–2.20(5H, m), 2.35(2H, t, J=7.2 Hz), 2.52(1H, m),3.82 (1H, m), 4.16(2H, s), 5.30–5.43(2H, m), 5.98(1H, d, J=7.2 Hz), 6.13(1H, dd, J=3.3 and 0.9 Hz), 6.32(1H, dd, J=3.3 and 1.8 Hz), 6.84(1H, d,J=3.6 Hz), 7.35(1H, dd, J=1.8 and 0.9 Hz), 7.37(1H, d, J=3.6 Hz). IR(CHCl₃): 3512, 3446, 3427, 2669, 1709, 1.643, 1545, 1506 cm⁻¹. [α]_(D)²²+69.6±1.1°(c=1.015, MeOH) Anal. (C₂₄H₂₉NO₄S.0.2H₂O) Calcd.(%): C,66.86; H, 6.87; N, 3.25; S, 7.44. Found(%): C, 66.75; H, 6.63; N, 3.32;S, 7.50.

Compound Number I-134

¹H-NMR(CDCl₃) δ: 1.07(1H, m), 1.19–1.29(2H, m), 1.45–1.60(2H, m),1.61–1.80(4H, m), 2.00–2.21(5H, m), 2.36(2H, t, J=7.2 Hz), 2.52(1H, m),3.81(1H, m), 3.96(2H, s), 5.29–5.42(2H, m), 5.96(1H, d, J=6.9 Hz), 6.30(1H, m), 6.80(1H, m), 7.32(1H, m), 7.35–7.39(2H, m). IR(CHCl₃): 3516,3446, 3427, 2663, 1709, 1643, 1545, 1506 cm⁻¹. [α]_(D)²¹+70.2±1.1°(c=1.007, MeOH) Anal. (C₂₄H₂₉NO₄S) Calcd.(%): C, 67.42; H,6.84; N, 3.28; S, 7.50. Found(%): C, 67.13; H, 6.57; N, 3.40; S, 7.40.

Compound Number I-135

¹H-NMR(CDCl₃) δ: 1.06(1H, m), 1.20–1.29(2H, m), 1.42–1.47(2H, m),1.58–1.82(4H, m), 2.00–2.15(5H, m), 2.35(2H, t, J=7.2 Hz), 2.52(1H, m),3.81 (1H, m), 4.41(2H, s), 5.29–5.41(2H, m), 5.96(1H, d, J=7.2 Hz), 6.91(1H, d, J=3.6 Hz), 7.11(1H, s), 7.25–7.35(3H, m), 7.39(1H, d, J=3.6 Hz),7.76 (1H, d, J=7.8 Hz). IR(CHCl₃): 3510, 3444, 3427, 2667, 1709, 1643,1543, 1508 cm⁻¹. [α]_(D) ²⁴+66.5±1.1°(c=1.012, MeOH) Anal.(C₂₈H₃₁NO₃S₂.0.5H₂O) Calcd.(%): C, 66.90; H, 6.42; N, 2.79; S, 12.76.Found(%): C, 66.99; H, 6.12; N, 2.81; S, 12.48.

Compound Number I-136

¹H-NMR(CDCl₃) δ: 1.07(1H, m), 1.20–1.42(2H, m), 1.44–1.49(2H, m),1.55–1.80(4H, m), 2.00–2.20(5H, m), 2.35(2H, t, J=7.2 Hz), 2.52(1H, m),3.81 (1H, m), 4.30(2H, s), 5.29–5.41(2H, m), 5.98(1H, d, J=7.8 Hz), 6.51(1H, d, J=0.6 Hz), 6.92(1H, d, J=3.9 Hz), 7.17–7.25(2H, m), 7.38–7.51(3H, m). IR (CHCl₃): 3514, 3444, 3427, 2669, 1709, 1643, 1545, 1508,1454 cm⁻¹. [α]_(D) ²³+63.8±1.0°(c=1.004, MeOH) Anal. (C₂₈H₃₁NO₄S.0.3H₂O)Calcd.(%): C, 69.62; H, 6.59; N, 2.90; S, 6.64. Found(%): C, 69.51; H,6.52; N, 2.92; S, 6.63.

Compound Number I-137

¹H-NMR(CDCl₃) δ: 1.05(1H, m), 1.18–1.29(2H, m), 1.40–1.48(2H, m),1.55–1.78(4H, m), 1.98–2.18(5H, m), 2.34(2H, t, J=7.2 Hz), 2.51(1H, m),3.81(1H, m), 4.17(2H, s), 5.29–5.42(2H, m), 5.98(1H, d, J=7.5 Hz), 6.81(1H, d, J=3.6 Hz), 7.29–7.46(6H, m), 7.52–7.60(41H, m). IR(CHCl₃): 3510,3446, 3427, 1741, 1709, 1643, 1543, 1506, 1489 cm⁻¹. [α]_(D)²³+59.4±1.0°(c=1.007, MeOH) Anal. (C₃₂H₃₅NO₃S.0.2H₂O) Calcd.(%): C,74.30; H, 6.90; N, 2.71; S, 6.20. Found(%): C, 74.24; H, 6.78; N, 2.97;S, 6.16.

Compound Number I-138

¹H-NMR(CDCl₃) δ: 1.04(1H, m), 1.17–1.29(2H, m), 1.39–1.47(2H, m),1.54–1.76(4H, m), 1.97–2.38(5H, m), 2.33(2H, t, J=7.5 Hz), 2.51(1H, m),3.80 (1H, m), 4.19(2H, s), 5.28–5.41(2H, m), 5.98(1H, d, J=7.5 Hz), 6.79(1H, d, J=3.6 Hz), 7.21(1H, d, J=7.8 Hz), 7.31–7.49(7H, m), 7.56(2H, m).IR (CHCl₃): 3512, 3446, 3427, 2669, 1741, 1709, 1643, 1543, 1506, 1479,1456 cm⁻¹. [α]_(D) ²⁴+59.2±1.0°(c=1.006 MeOH) Anal. (C₃₂H₃₅NO₃S.0.2H₂)Calcd.(%): C, 74.30; H, 6.90; N, 2.71; S, 6.20. Found(%): C, 74.26; H,6.92; N, 3.00; S, 6.20.

Compound Number I-139

¹H-NMR(CDCl₃) δ: 1.05(1H, m), 1.17–1.32(2H, m), 1.43–1.48(2H, m),1.58–1.80(4H, m), 2.02–2.24(5H, m), 2.34(2H, t, J=7.2 Hz), 2.58(1H, s),3.91(1H, m),4.11(2H, s), 5.30–5.44(2H, m), 6.11(1H, d, J=7.2 Hz),7.18–7.30(6H, m), 7.75(1H, d, J=8.4 Hz), 7.86(1H, s), 8.16(1H, s).IR(CHCl₃): 3516, 3430, 2665, 1741, 1709, 1651, 1513, 1494, 1454, 1435cm⁻¹. [α]_(D) ²⁴+45.6±0.9°(c=1.004, MeOH) Anal. (CO₃₀H₃₃NO₃S.0.1H₂O)Calcd.(%): C, 73.62; H, 6.84; N, 2.86; S, 6.55. Found(%): C, 73.57; H,6.71; N, 3.07; S, 6.30.

Compound Number I-140

¹H-NMR(CDCl₃) δ: 1.09(1H, m), 1.20–1.32(2H, m), 1.46–1.51(2H, m),1.58–1.78(4H, m), 2.02–2.24(5H, m), 2.35(2H, t, J=7.41 Hz), 2.60(1H, s),3.92(1H, m),4.10(2H, s), 5.32–5.46(2H, m), 6.14(1H, d, J=7.2 Hz),7.19–7.32(6H, m), 7.64(1H, s), 7.81(1H, s), 8.20(1H, d, J=8.4 Hz).IR(CHCl₃): 3516, 3438, 2669, 1709, 1651, 1516, 1494, 1406 cm⁻¹. [α]_(D)²⁴+53.0±0.9°(c=1.002, MeOH) Anal. (C₃₀H₃₃NO₃S) Calcd.(%): C, 73.89; H,6.82; N, 2.87; S, 6.58. Found(%): C, 73.57; H, 7.05; N, 3.08; S, 6.63.

Compound Number I-141

mp.54–56° C.; ¹-NMR(CDCl₃) δ: 0.97(1H, m), 1.10–1.43(4H, m), 1.53–1.72(4H, m), 1.97–2.15(5H, m), 2.31(2H, t, J=7.4 Hz), 2.45(1H, s), 3.83(1H,m), 4.39 and 4.52(each 1H, each d, J=16.5 Hz), 5.25–5.40(2H, m), 5.98(1H, d, J=7.5 Hz), 7.00–7.31(7H, m), 7.57(1H, s), 7.73(1H, d, J=7.5 Hz).IR (CHCl₃): 3514, 3433, 2671, 1709, 1655, 1512, 1454 cm⁻¹. [α]_(D)²⁵+76.7±1.2°(c=1.005, MeOH) Anal. (C₃₀H₃₃NO₃S.0.1H₂O) Calcd.(%): C,73.62; H, 6.84; N, 2.86; S, 6.55. Found(%): C, 73.45; H, 6.91; N, 3.21;S, 6.34.

Compound Number I-142

mp.118–119° C.; ¹H-NMR(CDCl₃) δ: 1.07(1H, m), 1.20–1.27(2H, m),1.42–1.46(2H, m), 1.55–1.73(4H, m), 1.99–2.12(5H, m), 2.33(2H, t, J=7.5Hz), 2.52(1H, s), 3.82(1H, m),3.93(2H, s), 5.29–5.42(2H, m), 6.10 (1H,d, J=7.2 Hz), 7.05(1H, d, J=0.9 Hz), 7.16–7.32(6H, m). IR(CHCl₃): 3516,3444, 3429, 2669, 1739, 1709, 1665, 1549, 1508, 1454 cm⁻¹. [α]_(D)²⁴+72.7±0.1.1°(c=1.001, MeOH) Anal. (C₂₆H₃₁NO₃S) Calcd.(%): C, 71.36; H,7.14; N, 3.20; S, 7.33. Found(%): C, 71.31; H, 7.27; N, 3.36; S, 7.31.

Compound Number I-143

¹H-NMR(CDCl₃) δ: 1.09(1H, m), 1.19–1.32(2H, m), 1.46–1.51(2H, m),1.58–1.78(4H, m), 2.02–2.24(5H, m), 2.35(2H, t, J=7.2 Hz), 2.60(1H, s),3.92(1H, m),4.24(²H, s), 5.32–5.47(2H, m), 6.14(1H, d, J=7.5 Hz),7.18–7.30(6H, m), 7.43(1H, t, J=7.8 Hz), 7.83(1H, s), 8.17(1H, d, J=7.8Hz). IR(CHCl₃): 3516, 3438, 2671, 1709, 1651, 1518, 1495, 1454 cm⁻¹.[α]_(D) ²⁵+62.8±1.0°(c=1.011, MeOH) Anal. (C₃₀H₃₃NO₃S.0.1H₂O) Calcd.(%):C, 73.62; H, 6.84; N, 2.86; S, 6.55. Found(%): C, 73.52; H, 6.87; N,3.13; S, 6.47.

Compound Number I-144

¹H-NMR(CDCl₃) δ: 1.05(1H, m), 1.23–1.29(2H, m), 1.41–1.49(2H, m),1.58–1.77(4H, m), 2.00–2.21(5H, m), 2.35(2H, t, J=7.2 Hz), 2.52(1H, m),3.81 (1H, m), 4.05(2H, s), 5.12(2H, s), 5.29–5.42(2H, m), 5.94(1H, d,J=7.8 Hz), 6.76(1H, d, J=3.9 Hz), 6.90–6.98(31H, m), 7.32–7.45 (6H, m).IR (CHCl₃): 3516, 3446, 3427, 1741, 1709, 1643, 1543, 1510, 1456, 1273cm⁻¹. [α]_(D) ²³+53.7±0.9°(c=1.006, MeOH) Anal. (C₃₃H₃₆FNO₄S.0.2H₂O)Calcd.(%): C, 70.11; H, 6.49; N, 2.48; S, 5.67; F, 3.36. Found(%): C,70.00; H, 6.44; N, 2.50; S, 5.75; F, 3.32.

Compound Number I-145

mp.136–137° C.; ¹H-NMR(CDCl₃) δ: 1.06(1H, m), 1.23–1.29(2H, m),1.41–1.49(2H, m), 1.58–1.77(4H, m), 2.00–2.21(5H, m), 2.35(2H, t, J=7.2Hz), 2.52(1H, m), 3.78(1H, m), 4.05(2H, s), 5.29–5.42(2H, m), 5.93 (1H,d, J=10.8 Hz), 6.77(1H, d, J=3.6 Hz), 6.88–6.98(3H, m), 7.36 (1H, d,J=3.6 Hz). IR (Nujol): 3377, 3101, 2752, 1703, 1618, 1601, 1550, 1518cm⁻¹. [α]_(D) ²³+64.2±1.0°(c=1.009, MeOH) Anal. (C₂₆H₃₀FNO₄S) Calcd.(%):C, 66.23; H, 6.41; N, 2.97; S, 6.80; F, 4.03. Found(%): C, 66.15; H,6.38; N, 2.94; S, 6.76; F, 3.94.

Compound Number I-146

¹H-NMR(CDCl₃) δ: 1.06(1H, m), 1.20–1.29(2H, m), 1.41–1.46(2H, m),1.61–1.81(4H, m), 2.00–2.16(5H, m), 2.35(2H, t, J=7.2 Hz), 2.51(1H, m),3.79 (1H, m), 4.03(2H, s), 5.08(2H, s), 5.29–5.40(2H, m), 5.63(1H, brs),5.93 (1H, d, J=7.5 Hz), 6.70(1H, dd, J=2.1 and 8.4 Hz), 6.77 (1H, d,J=3.9 Hz), 6.83 (1H, d, J=5.7 Hz). 6.86(1H, d, J=8.4 Hz), 7.36–7.41(6H,m). IR(CHCl₃): 3539, 3446, 3425, 1741, 1709, 1641, 1543, 1508, 1475,1273 cm⁻¹. [α]_(D) ²³+53.8±0.9°(c=1.003, MeOH) Anal. (C₃₃H₃₇NO₅S.0.5H₂O)Calcd.(%): C, 69.69; H, 6.73; N, 2.46; S, 5.64. Found(%): C, 69.68; H,6.85; N, 2.68; S, 5.76.

Compound Number I-147

mp.150–151° C.; ¹H-NMR(CDCl₃) δ: 1.06(1H, m), 1.20–1.29(2H, m),1.41–1.46(2H, m), 1.58–1.79(4H, m), 2.00–2.16(5H, m), 2.35(2H, t, J=7.2Hz), 2.51(1H, m), 3.79(1H, m), 3.86(3H, s), 4.06(2H, s), 5.29–5.41 (2H,m), 5.56 (1H, brs), 5.93(1H, d, J=8.4 Hz), 6.72–6.77(3H, m), 6.87 (1H,d, J=8.1 Hz), 7.37(1H, d, J=3.6 Hz). IR(Nujol): 3452, 3361, 3130, 1.743,1707, 1620, 1599, 1550, 1522, 1286 cm⁻¹. [α]_(D) ²³+62.6±1.0°(c=1.002,MeOH) Anal. (C₂₇H₃₃NO₅S) Calcd.(%): C, 67.05; H, 6.88; N, 2.90; S, 6.63.Found(%): C, 67.20; H, 7.04; N, 2.98; S, 6.58.

Compound Number I-148

¹H-NMR(CDCl₃) δ: 1.07(1H, m), 1.19–1.31(2H, m), 1.41–1.50(2H, m),1.56–1.81 (4H, m), 1.99–2.21(5H, m), 2.35(2H, t, J=7.2 Hz), 2.53(1H, m),2.95–3.00 (2H, m), 3.10–3.15(2H, m),3.83(1H, m), 5.31–5.44(2H, m), 6.02(1H, d, J=7.2 Hz), 6.70(1H, d, J=3.9 Hz), 7.15–7.32(5H, m), 7.33(1H, d,J=3.9 Hz). IR(CHCl₃): 3510, 3446, 3429, 2671, 1741, 1709, 1641, 1543,1506, 1456 cm⁻¹. [α]_(D) ²³+68.4±1.1°(c=1.004, MeOH) Anal.(C₂₇H₃₃NO₃S.0.1H₂O) Calcd.(%): C, 71.52; H, 7.38; N, 3.09; S, 7.07.Found(%): C, 71.35; H, 7.37; N, 3.19; S, 7.19.

Compound Number I-149

¹H-NMR(CDCl₃) δ: 1.07(1H, m), 1.19–1.32(2H, m), 1.41–1.50(2H, m),1.56–1.81 (4H, m), 1.99–2.23(5H, m), 2.36(2H, t, J=7.2 Hz), 2.43(3H, s),2.53 (1H, m), 3.05–3.19(4H, m), 3.83(1H, m), 5.31–5.44(2H, m), 6.00(1H,d, J=6.9 Hz), 6.23–6.56(2H, m), 6.75 and 7.34(each 1H, each d, eachJ=3.6 Hz). IR (CHCl₃): 3510, 3446, 3429, 2669, 1709, 1641, 1543, 1506,1458 cm⁻¹. [α]_(D) ²³+64.6±1.0°(c=1.014, MeOH) Anal.(C₂₆H₃₃NO₃S₂.0.1H₂O) Calcd.(%): C, 65.96; H, 7.07; N, 2.96; S, 13.54.Found(%): C, 65.87; H, 7.03; N, 3.02; S, 13.50.

Compound Number I-150

¹H-NMR(CDCl₃) δ: 1.07(1H, m), 1.19–1.31(2H, m), 1.41–1.50(2H, m),1.56–1.80(4H, m), 1.99–2.20(5H, m), 2.35(2H, t, J=7.5 Hz), 2.53(1H, m),3.18(3H, s), 3.83(1H, m), 5.31–5.44(2H, m), 6.05(1H, d, J=7.2 Hz), 6.74(1H, d, J=3.6 Hz), 6.79(1H, m), 6.91(1H, dd, J=3.6 and 5.4 Hz), 7.13(1H,dd, J=1.2 and 5.4 Hz), 7.34(1H, d, J=3.6 Hz). IR(CHCl₃): 3516, 34446,3429, 2669, 1709, 1641, 1543, 1506 cm⁻¹. [α]_(D) ²⁴30 66.1±1.0°(c=1.019,MeOH) Anal. (C₂₅H₃₁NO₃S₂) Calcd.(%): C, 65.61; H, 6.83; N, 3.06; S,14.01. Found(%): C, 65.47; H, 6.89; N, 3.12; S, 13.82.

Compound Number I-151

¹H-NMR(CDCl₃) δ: 1.09(1H, m), 1.20–1.32(2H, m), 1.42–1.51(2H, m),1.57–1.81(4H, m), 2.00–2.22(5H, m), 2.33(2H, t, J=7.5 Hz), 2.56(1H, m),2.99–3.05(2H, m), 3.11–3.17(2H, m), 3.88(1H, m), 5.30–5.44(2H, m), 6.22(1H, d, J=7.2 Hz), 6.74(1H, m), 6.89(1H, dd, J=3.3 and 5.1 Hz), 7.11(1H,dd, J=1.2 and 5.1 Hz), 7.23 and 7.67(each 2H, each d, each J=8.1 Hz). IR(CHCl₃): 3516, 3448, 2665, 1709, 1651, 1523, 1496 cm⁻¹. [α]_(D)²⁴+71.8±1.1°(c=1.009, MeOH) Anal. (C₂₇H₃₃NO₃S) Calcd.(%): C, 71.81; H,7.37; N, 3.10; S, 7.10. Found(%): C, 71.68; H, 7.40; N, 3.18; S, 6.96.

Compound Number I-152

¹H-NMR(CDCl₃) δ: 1.07(1H, m), 1.19–1.31(2H, m), 1.42–1.50(2H, m),1.56–1.81(4H, m), 2.00–2.21(5H, m), 2.36(2H, t, J=7.2 Hz), 2.53(1H, m),2.92–2.97(2H, m), 3.07–3.12(2H, m), 3.83(1H, m), 5.31–5.44(2H, m), 5.99(1H, d, J=7.2 Hz), 6.68(1H, d, J=3.6 Hz), 6.92–7.00(2H, m),7.08–7.15(2H, m), 7.32(1H, d, J=3.6 Hz). IR(CHCl₃): 3516, 3446, 3429,1741, 1709, 1641, 1543, 1510, 1458 cm⁻¹. [α]_(D) ²³+64.1±1.0°(c=1.012,MeOH) Anal. (C₂₇H₃₂FNO₃S) Calcd.(%): C, 69.06; H, 6.87; N, 2.98; S,6.83; F, 4.05. Found(%): C, 68.92; H, 6.90; N, 3.03; S, 6.81; F, 4.02.

Compound Number I-153

¹H-NMR(CDCl₃) δ: 1.05(1H, m), 1.19–1.29(2H, m), 1.41–1.46(2H, m),1.56–1.78(4H, m), 2.00–2.19(5H, m), 2.29(6H, s), 2.34(2H, t, J=7.5 Hz),2.51(1H, m), 3.81(1H, m), 4.05(2H, s), 5.29–5.42(2H, m), 5.96(1H, d,J=7.5 Hz), 6.77(1H, td, J=0.9 and 3.6 Hz), 6.85(2H, s), 6.88(1H, s),7.37 (1H, d, J=3.6 Hz). IR(CHCl₃): 3516, 3446, 3427, 1739, 1709, 1641,1606, 1543, 1506, 1458 cm⁻¹. [α]_(D) ²³+64.6±1.0°(c=1.004, MeOH) Anal.(C₂₈H₃₅NO₃S.0.1H₂O) Calcd.(%): C, 71.94; H, 7.59; N, 3.00; S, 6.86.Found(%): C, 71.87; H, 7.52; N, 3.31; S, 6.94.

Compound Number I-154

¹H-NMR(CDCl₃) δ: 1.05(1H, m), 1.18–1.29(2H, m), 1.41–1.46(2H, m),1.56–1.78 (4H, m), 2.00–2.19(5H, m), 2.34(2H, t, J=7.5 Hz), 2.51(1H, m),3.81(1H, m), 4.10(2H, s), 5.29–5.42(2H, m), 5.98(1H, d, J=7.2 Hz), 6.75(1H, td, J=0.9 and 3.9 Hz), 6.97–7.03(2H, m), 7.17–7.22(2H, m), 7.36(1H,d, J=3.9 Hz). IR(CHCl₃): 3512, 3446, 3427, 1741, 1709, 1643, 1543, 1508cm⁻¹. [α]_(D) ²⁴+66.1±1.1°(c=1.008, MeOH) Anal. (C₂₆H₃₀FNO₃S) Calcd.(%):C, 68.54; H, 6.64; N, 3.07; S, 7.04; F, 4.17. Found(%): C, 68.41; H,6.70; N, 3.19; S, 6.90; F,3.98.

Compound Number I-155

¹H-NMR(CDCl₃) δ: 1.05(1H, m), 1.19–1.29(2H, m), 1.42–1.46(2H, m),1.58–1.78(4H, m), 2.00–2.17(5H, m), 2.35(2H, t, J=7.5 Hz), 2.52(1H, m),3.81 (1H, m), 4.19(2H, s), 5.29–5.42(2H, m), 5.97(1H, d, J=7.8 Hz), 6.75(1H, td, J=0.9 and 3.6 Hz), 7.34–7.37(3H, m), 7.56–7.59(2H, m). IR(CHCl₃): 3512, 3444, 3427, 1741, 1709, 1643, 1543, 1506, 1325, 1167,1130, 1066 cm⁻¹. [α]_(D) ²⁴+60.3±1.0°(c=1.001, MeOH) Anal.(C₂₇H₃₀F₃NO₃S) Calcd.(%): C, 64.14; H, 5.98; N, 2.77; S, 6.34; F, 11.27.Found(%): C, 64.16; H, 6.04; N, 3.02; S, 6.19; F, 11.17.

Compound Number I-156

mp.66–70° C.; ¹H-NMR(CDCl₃) δ: 1.11(1H, m), 1.22–1.30(2H, m),1.43–1.50(2H, m), 1.60–1.78(4H, m), 2.03–2.22(5H, m), 2.36(2H, t, J=7.5Hz), 2.54(1H, m), 3.87(1H, m), 4.08(2H, s), 5.31–5.45(2H, m), 6.21 (1H,d, J=7.2 Hz), 7.18–7.32(6H, m), 7.60(1H, d, J=0.9 Hz), 7.70(1H, d, J=0.6Hz), 7,74 (1H, d, J=8.1 Hz). IR(KBr): 3338, 1707, 1616, 1556, 1537 cm⁻¹.[α]_(D) ²³+97.2±1.4°(c=1.016, MeOH) Anal. (C₃₀H₃₃NO₃S.0.3H₂O) Calcd.(%):C, 73.08; H, 6.87; N, 2.84; S, 6.50. Found(%): C, 73.19; H, 7.11; N,2.98; S, 6.32.

Compound Number I-157

¹H-NMR(CDCl₃) δ: 1.03(1H, m), 1.17–1.29(2H, m), 1.38–1.47(2H, m),1.55–1.76(4H, m), 1.97–2.18(5H, m), 2.33(2H, t, J=7.5 Hz), 2.50(1H, m),3.80 (1H, m), 4.29(2H, s), 5.28–5.40(2H, m), 5.94(1H, d, J=7.5 Hz), 6.81(1H, d, J=3.9 Hz), 7.32–7.39(2H, m), 7.42–7.50(2H, m), 7.69(1H, s),7.77–7.83 (3H, m). IR(CHCl₃): 3516, 3446, 3427, 2665, 1739, 1709, 1643,1543, 1506, 1458 cm⁻¹. [α]_(D) ²³+62.8±1.0°(c=1.005, MeOH) Anal.(C₃₀H₁₂NO₃S.0.2H₂O) Calcd.(%): C, 73.35; H, 6.85; N, 2.85; S, 6.53.Found(%): C, 73.36; H, 6.84; N, 3.19; S, 6.55.

Compound Number I-158

¹H-NMR(CDCl₃) δ: 1.07(1H, m), 1.20–1.32(2H, m), 1.42–1.50(2H, m),1.57–1.84 (4H, m), 2.00–2.23(5H, m), 2.36(2H, t, J=7.5 Hz), 2.53(1H, m),2.95–3.00(2H, m), 3.06–3.12(2H, m), 3.82(1H, m),3.83(3H, s), 5.30–5.43(2H, m), 5.95(1H, d, J=6.9 Hz), 6.73(1H, d, J=3.6 Hz), 6.84–6.89(2H, m),7.09 (1H, dd, J=1.5 and 7.5 Hz), 7.20(1H, dt, J=1.5 and 7.5 Hz),7.34(1H, d, J=3.6 Hz). IR(Nujol): 3367, 3221, 3186, 3091, 3055, 2654,1711, 1631, 1566, 1541, 1321 cm⁻¹. [α]_(D) ²⁵+61.3±1.020 (c=1.003, MeOH)Anal. (C₂₈H₃₅NO₄S) Calcd.(%): C, 69.82; H, 7.32; N, 2.91; S, 6.66.Found(%): C, 69.93; H, 7.48; N, 3.09; S, 6.54.

Compound Number I-159

¹H-NMR(CDCl₃) δ: 1.07(1H, m), 1.18–1.30(2H, m), 1.40–1.50(2H, m),1.54–1.78(4H, m), 1.98–2.21(5H, m), 2.33(2H, t, J=7.2 Hz), 2.53(1H, m),2.94–3.03 (2H, m), 3.06–3.15(2H, m), 3.83(1H, m), 5.29–5.43(2H, m), 6.12(1H, d, J=7.5 Hz), 6.72(1H, d, J=3.6 Hz), 6.77–6.83(2H, m),7.04–7.08(2H, m), 7.36(1H, d, J=3.6 Hz). IR(CHCl₃): 3599, 3444, 3425,3195, 1709, 1635, 1543, 1508, 1456 cm⁻¹. [α]_(D) ²⁵+64.8±1.0°(c=1.006,MeOH) Anal. (C₂₇H₃₃NO₄S.0.2H₂O) Calcd.(%): C, 68.82; H, 7.14; N, 2.97;S, 6.80. Found(%): C, 68.81; H, 7.10; N, 3.03; S, 6.88.

Compound Number I-160

mp.139–141° C.; ¹H-NMR(CDCl₃) δ: 1.12(1H, m), 1.25–1.31(2H, m),1.45–1.51(2H, m), 1.60–1.78(4H, m), 2.02–2.22(5H, m), 2.35(2H, t, J=7.5Hz), 2.57 (1H, m), 3.87(1H, m), 4.09(2H, s), 5.31–5.45(2H, m), 6.22 (1H,d, J=7.2 Hz), 7.19–7.33(6H, m), 7.63(1H, m), 7.71(1H, d, J=8.7 Hz),7,73(1H, s). IR (KBr): 3338, 1705, 1616, 1560, 1537 cm⁻¹. [α]_(D)²⁵+92.1±1.3°(c=1.006, MeOH) Anal. (C₃₀H₃₃NO₃S) Calcd.(%): C, 73.89; H,6.82; N, 2.87; S, 6.58. Found(%): C, 73.69; H, 6.75; N, 2.91; S, 6.58.

Compound Number I-161

¹H-NMR(CDCl₃) δ: 1.12(1H, m), 1.25–1.31(2H, m), 1.47–1.51(2H, m),1.60–1.76(4H, m), 2.03–2.20(5H, m), 2.36(2H, t, J=7.2 Hz), 2.57(1H, m),3.87 (1H, m), 4.08(2H, s), 5.31–5.45(2H, m), 6.22(1H, d, J=7.5 Hz), 6.90(1H, dd, J=1.2 and 4.8 Hz), 6.93(1H, m), 7.25–7.29(2H, m), 7.61 and 7.71(each 1H, each s), 7.75(1H, d, J=8.4 Hz). IR(CHCl₃): 3512, 3444, 3423,2671, 1709, 1649, 1531, 1502 cm⁻¹. [α]_(D) ²⁵+96.1±1.4°(c=1.005, MeOH)Anal. (C₂₈H₃₁NO₃S₂) Calcd.(%): C, 68.12; H, 6.33; N, 2.84; S, 12.99.Found(%): C, 67.89; H, 6.32; N, 2.88; S, 12.88.

Compound Number I-162

¹H-NMR(CDCl₃) δ: 1.12(1H, m), 1.24–1.31(2H, m), 1.45–1.51(2H, m),1.60–1.78(4H, m), 2.03–2.22(5H, m), 2.36(2H, t, J=7.2 Hz), 2.57(1H, m),3.87(1H, m), 4.25(2H, s), 5.31–5.45(2H, m), 6.25(1H, d, J=7.2 Hz), 6.81(1H, m), 6.93(1H, dd, J=3.3 and 5.4 Hz), 7.15(1H, dd, J=1.5 and 5.4 Hz),7.31 (1H, dd, J=1.5 and 8.1 Hz), 7.65 and 7.71(each 1H, each s),7.76(1H, d, J=8.1 Hz). IR(CHCl₃): 3516, 3444, 3423, 1741, 1709, 1649,1531, 1502 cm⁻¹. [α]_(D) ²⁵+98.5±1.4°(c=1.007, MeOH) Anal.(C₂₈H₃₁NO₃S₂.0.1H₂O) Calcd.(%): C, 67.87; H, 6.35; N, 2.83; S, 12.94.Found(%): C, 67.83; H, 6.29; N, 3.00; S, 12.99.

Compound Number I-163

mp.114–115° C.; ¹NMR(CDCl₃) δ: 1.09(1H, m), 1.20–1.30(2H, m), 1.40–1.49(2H, m), 1.55–1.77(4H, m), 1.99–2.19(5H, m), 2.34(2H, t, J=7.2 Hz),2.53(1H, m, 3.83(1H, m), 4.12(2H, s), 5.30–5.43(2H, m), 6.14 (1H, d,J=7.5 Hz), 6.81 and 6.93(each 1H, each m), 7.14–7.17(2H, m), 7.37(1H, d,J=1.8 Hz). IR (CHCl₃): 3516, 3444, 3428, 2671, 1709, 1645, 1550, 1508,1435 cm⁻¹. [α]_(D) ²⁵+71.6±1.1°(c=1.002, MeOH) Anal.(C₂₄H₂₉NO₃S₂.0.1H₂O) Calcd.(%): C, 64.72; H, 6.61; N, 3.14; S, 14.40.Found(%): C, 64.50; H, 6.54; N, 3.24; S, 14.45.

Compound Number I-164

¹H-NMR(CDCl₃) δ: 1.08(1H, m), 1.20–1.31(2H, m), 1.41–1.49(2H, m),1.56–1.77(4H, m), 1.99–2.19(5H, m), 2.34(2H, t, J=7.211 Hz), 2.53(1H,m), 3.83(1H, 3.94(2H, s), 5.30–5.43(2H, m), 6.08(1H, d, J=6.9 Hz), 6.91and 6.95 (each 1H, each m), 7.08(1H, d, J=1.5 Hz), 7.27(1H, m), 7.34(1H,d, J=1.5 Hz). IR(CHCl₃): 3512. 3444, 3429, 1739, 1709, 1644, 1550, 1508cm⁻¹. [α]_(D) ²⁵+69.7±1.1°(c=1.000, MeOH) Anal. (C₂₄H₂₉NO₃S₂.0.2H₂O)Calcd.(%): C, 64.45; H, 6.63; N, 3.13; S, 14.34. Found(%): C, 64.37; H,6.49; N, 3.16; S, 14.41.

Compound Number I-165

¹H-NMR(CDCl₃) δ: 1.08(1H, m), 1.19–1.31(2H, m), 1.41–1.51(2H, m),1.55–1.74(4H, m), 1.99–2.16(5H, m), 2.34(2H, t, J=7.2 Hz), 2.53(1H, m),3.73(2H, s), 3.83(1H, m), 5.30–5.42(2H, m), 6.15(1H, d, J=6.6 Hz), 6.25,7.10 and 7.24(each 1H, each s), 7.35–7.38(2H, m). IR(CHCl₃): 3510, 3444,3429, 2669, 1709, 1645, 1550, 1508 cm⁻¹. [α]_(D) ²⁵+71.635 1.1°(c=1.008,MeOH) Anal. (C₂₄H₂₉NO₄S.0.2H₂O) Calcd.(%): C, 66.85; H, 6.78; N, 3.25;S, 7.44. Found(%): C, 66.94; H, 6.81; N, 3.26; S, 7.38.

Compound Number I-166

¹H-NMR(CDCl₃) δ: 1.02(1H, m), 1.15–1.27(2H, m), 1.36–1.45(2H, m),1.53–1.76(4H, m), 1.96–2.14(5H, m), 2.32(2H, t, J=7.2 Hz), 2.49(1H, m),3.78 (1H, m), 4.58(2H, s), 5.27–5.39(2H, m), 5.92(1H, d, J=7.2 Hz), 6.73and 7.32(each 1H, each d, each J=3.9 Hz), 7.37–7.51(4H, m), 7.80(1H, d,J=7.5 Hz), 7.87 and 7.97(each 1H, each m). IR(CHCl₃): 3516, 3446, 3427,2669, 1739, 1709, 1641, 1543, 1508, 1458 cm⁻¹. [α]_(D)^(25.5)+62.8±1.0°(c=1.012, MeOH) Anal. (C₃₀H₃₃NO₃S.0.1H₂O) Calcd.(%): C,73.62; H, 6.84; N, 2.86; S, 6.55. Found(%): C, 73.35; H, 6.54; N, 3.06;S, 6.51.

Compound Number I-167

mp.129–130° C.; ¹H-NMR(CDCl₃) δ: 1.04(1H, m), 1.16–1.28(2H, m),1.38–1.46(2H, m), 1.54–1.73(4H, m), 1.97–2.15(5H, m), 2.31(2H, t, J=7.2Hz), 2.51(1H, m), 3.81(1H, m), 4.37(2H, s), 5.28–5.41(2H, m), 6.04 (1H,d, J=7.5 Hz), 6.97(1H, s), 7.30–7.50(5H, m), 7.77(1H, d, J=8.1 Hz), 7.86and 7.94(each 1H, each m). IR(CHCl₃): 3514, 3444, 3427, 1739, 1709,1645, 1549, 1508 cm⁻¹. [α]_(D) ²⁴+59.4±1.0°(c=1.011, MeOH) Anal.(C₃₀H₃₃NO₃S) Calcd.(%): C, 73.89; H, 6.82; N, 2.87; S, 6.58. Found(%):C, 73.85; H, 6.90; N, 2.85; S, 6.81.

Compound Number I-168

¹H-NMR(CDCl₃) δ: 1.10(1H, m), 1.21–1.33(2H, m), 1.47–1.52(2H, m),1.59–1.80 (4H, m), 2.04–2.27(5H, m), 2.36(2H, t, J=7.5 Hz), 2.61(1H, m),3.93(1H, m), 4.42(2H, s), 5.33–5.47(2H, m), 6.13(1H, d, J=7.5 Hz), 6.88(1H, m), 6.92(1H, m), 7.15(1H, dd, J=1.2 and 5.1 Hz), 7.28(1H, d, J=7.5Hz), 7.43 (1H, d, J=8.1 Hz), 7.84(1H, s), 8.20(1H, d, J=8.1 Hz).IR(CHCl₃): 3512, 3438, 1709, 1651, 1518, 1495 cm⁻¹. [α]_(D)²⁵+61.6±1.0°(c=1.003, MeOH) Anal. (C₂₈H₃₁NO₃S₂) Calcd.(%): C, 68.12; H,6.33; N, 2.84; S, 12.99. Found(%): C, 67.83; H, 6.28; N, 2.96; S, 12.76.

Compound Number I-169

¹H-NMR(CDCl₃) δ: 1.10(1H, m), 1.22–1.32(2H, m), 1.46–1.51(2H, m),1.58–1.76(4H, m), 2.02–2.24(5H, m), 2.35(2H, t, J=7.2 Hz), 2.60(1H, m),3.92 (1H, m), 4.23(2H, s), 5.32–5.47(2H, m), 6.18(1H, d, J=8.1 Hz), 6.92(1H, dd, J=1.2 and 4.8 Hz), 7.01(1H, m), 7.20–7.25(2H, m), 7.41(1H, t,J=8.1 Hz), 7.84(1H, s), 8.18(1H, d, J=7.5 Hz). IR (CHCl₃): 3510, 3438,2667, 1709, 1651, 1518, 1495 cm⁻¹. [α]_(D) ²⁵+61.3±1.0°(c=1.006, MeOH)Anal. (C₂₈H₃₁NO₃S₂) Calcd.(%): C, 68.12; H, 6.33; N, 2.84; S, 12.99.Found(%): C, 67.94; H, 6.30; N, 2.97; S, 12.87.

Compound Number I-170

¹H-NMR(CDCl₃) δ: 1.10(1H, m), 1.21–1.33(2H, m), 1.47–1.52(2H, m),1.59–1.79(4H, m), 2.03–2.27(5H, m), 2.36(2H, t, J=7.5 Hz), 2.61(1H, m),3.93 (1H, m), 4.03(2H, s), 5.33–5.48(2H, m), 6.15(1H, d, J=7.2 Hz), 7.23(1H, d, J=7.2 Hz), 7.29(1H, m), 7.35(1H, t, J=1.5 Hz), 7.42(1H, t, J=7.8Hz), 7.85 (1H, s), 8.18(1H, (c, J=7.8 Hz). IR (CHCl₃): 3518, 3438, 2663,1739, 1709, 1651, 1518, 1496 cm⁻¹. [α]_(D) ²⁵+60.3±1.0®(c=1.002, MeOH)Anal. (C₂₈H₃₁NO₄S.0.1H₂O) Calcd.(%): C, 70.15; H, 6.56; N, 2.92; S,6.69. Found(%): C, 70.03; H, 6.49; N, 2.92; S, 6.69.

Compound Number I-171

¹H-NMR(CDCl₃) δ: 1.05(1H, m), 1.18–1.28(2H, m), 1.41–1.46(2H, m),1.56–1.79(4H, m), 2.00–2.15(5H, m), 2.34(2H, t, J=7.2 Hz), 2.45(3H, s),2.50(1H, m), 3.80(1H, m), 4.25(2H, s), 5.29–5.42(2H, m), 5,95(1H, d,J=7.5 Hz), 6.78(1H, d, J=3.6 Hz), 7.11–7.27(4H, m), 7.36(1H, d, J=3.6Hz). IR(CHCl₃): 3512, 3446, 3427, 2669, 1739, 1709, 1643, 1543, 1506cm⁻¹. [α]_(D) ^(23.5)+^(62.8±1.0)°(c=1.005, MeOH) Anal. (C₂₇H₃₃NO₃S₂)Calcd.(%): C, 67.05; H, 6.88; N, 2.90; S, 13.26. Found(%): C, 66.94; H,7.05; N, 3.00; S, 13.14.

Compound Number I-172

¹H-NMR(CDCl₃) δ: 1.07(1H, m), 1.19–1.29(2H, m), 1.41–1.46(2H, m),1.57–1.78(4H, m), 2.01–2.19(5H, m), 2.34(2H, t, J=7.5 Hz), 2.51(1H, m),2.90(3H, s), 3.80(1H, m), 4.68(2H, s), 5.29–5.43(2H, m), 6.02(1H, d,J=7.5 Hz), 6.84(1H, td, J=0.9 and 3.9 Hz), 7.37(1H,d, J=3.9 Hz),7.42–7.51 (2H, m), 7.62(1H, dt, J=1.5 and 7.5 Hz), 8.08(1H, dd, J=1,5and 7.5 Hz). IR(CHCl₃): 3518, 3444, 3427, 1709, 1643, 1543, 1508, 1311,1153 cm⁻¹. [α]_(D) ^(23.5)+59.3±1.0°(c=1.007, MeOH) Anal.(C₂₇H₃₃NO₅S₂.0.2H₂O) Calcd.(%): C, 62.45; H, 6.48; N, 2.70; S, 12.35.Found(%): C, 62.47; H, 6.60; N, 2.73; S, 12.36.

Compound Number I-173

¹H-NMR(CDCl₃) δ: 1.13(1H, m), 1.23–1.36(2H, m), 1.43–1.80(6H, m),2.03–2.24(5H, m), 2.36(2H, t, J=7.2 Hz), 2.60(1H, m), 3.91(1H, m), 3.93(2H, s), 5.31–5.46(2H, m), 6.31(1H, d, J=7.2 Hz), 7.32–7.42(2H, m), 7.57(1H, d, J=6.9 Hz), 7.73–7.82(3H, m), 7.94(1H, s). IR(CHCl₃): 3516, 3446,2665, 1709, 1649, 1616, 1514, 1481, 1468 cm⁻¹. [α]_(D)²⁴+100.7±1.4°(c=1.008, MeOH) Anal. (C₂₈H₃₁NO₃.0.2H₂O) Calcd.(%): C,77.64; H, 7.31; N, 3.23. Found(%): C, 77.64; H, 7.57; N, 3.29.

Compound Number I-174

¹H-NMR(CDCl₃) δ: 1.06(1H, m), 1.19–1.28(2H, m), 1.40–1.47(2H, m),1.57–1.78(4H, m), 1.99–2.18(5H, m), 2.35(2H, t, J=7.4 Hz), 2.51(1H, s),3.21(2H, t, J=8.7 Hz), 3.81(1H, m), 4.01(2H, s), 4.58(2H, t, J=8.7 Hz),5.29–5.42 (2H, m), 6.02(1H, d, J=7.5 Hz), 6.80(1H, d, J=3.9 Hz),7.06(1H, d, J=1.8 Hz), 7.18(1H, d, J=1.8 Hz), 7.36(1H, d, J=3.9 Hz). IR(CHCl₃): 3512, 3446, 3427, 2669, 1709, 1641, 1543, 1506, 1477, 1460,1173 cm⁻¹. [α]_(D) ²⁵+53.8±0.9°(c=1.007, MeOH) Anal.(C₂₈H₃₂BrNO₄S.0.1H₂O) Calcd.(%): C, 60.02; H, 5.79; Br, 14.26; N, 2.50;S, 5.72. Found(%): C, 59.87; H, 5.68; Br, 14.13; N, 2.59; S, 5.71.

Compound Number I-175

¹H-NMR(CDCl₃) δ: 1.12(1H, m), 1.23–1.31(2H, m), 1.44–1.51(2H, m),1.60–1.78(4H, m), 2.03–2.28(5H, m), 2.36(2H, t, J=7.4 Hz), 2.56(1H, s),3.87(1H, m),4.21(2H, s), 5.31–5.45(2H, m), 6.21(1H, d, J=7.2 Hz),7.18–7.37(7H, m), 7.70(1H, d, J=7.2 Hz), 7.80(1H, s). IR(CHCl₃): 3514,3444, 3423, 2667, 1709, 1649, 1537, 1502, 1454 cm⁻¹. [α]_(D)²⁵+78.2±1.2°(c=1.002, MeOH) Anal. (C₃₀H₃₃BrNO₃S.0.1H₂O) Calcd.(%): C,73.62; H, 6.84; N, 2.86; S, 6.55. Found(%): C, 73.49; H, 6.88; N, 2.89;S, 6.57.

Compound Number I-176

¹H-NMR(CDCl₃) δ: 1.12(1H, m), 1.23–1.32(2H, m), 1.44–1.51(2H, m),1.61–1.78(4H, m), 2.03–2.28(5H, m), 2.36(2H, t, J=7.4 Hz), 2.57(1H, s),3.88 (1H, m),4.21(2H, s), 5.31–5.45(2H, m), 6.22(1H, d, J=7.2 Hz), 6.94(1H, dd, J=1.5 and 4.8 Hz), 7.04(1H, m), 7.21–7.25(2H, m), 7.35(1H, dd,J=7.2 and 7.8 Hz), 7.71(1H, d, J=7.2 Hz), 7.80(1H, s). IR(CHCl₃): 3512,3444, 3423, 2669, 1709, 1647, 1539, 1504 cm⁻¹. [α]_(D)²⁵+77.1±1.2°(c=1.002, MeOH) Anal. (C₂₈H₃₁NO₃S₂.0.2H₂O) Calcd.(%): C,67.63; H, 6.36; N, 2.82; S, 12.90. Found(%): C, 67.57; H, 6.34; N, 2.97;S, 12.98.

Compound Number I-177

¹H-NMR(CDCl₃) δ: 1.12(1H, m), 1.25–1.32(2H, m), 1.44–1.51(2H, m),1.60–1.78(4H, m), 2.03–2.28(5H, m), 2.31(3H, s), 2.36(2H, t, J=7.2 Hz),2.56 (1H, s),3.87(1H, m),4.17(2H, s), 5.31–5.45(2H, m), 6.22(1H, d,J=7.2 Hz), 7.09 and 7.15(each 2H, each d, J=8.1 Hz), 7.19(1H, d, J=7.2Hz), 7.34(1H, dd, J=7.2 and 7.8 Hz), 7.69(1H, d, J=7.8 Hz), 7.79(1H, s).IR (CHCl₃): 3510, 3444, 3423, 2669, 1709, 1647, 1537, 1504 cm⁻¹. [α]_(D)²⁵+75.9±1.2°(c=1.004, MeOH) Anal. (C₃₁H₃₅NO₃S) Calcd.(%): C, 74.22; H,7.03; N, 2.79; S, 6.39. Found(%): C, 73.93; H, 7.13; N, 2.91; S, 6.38.

Compound Number I-178

¹H-NMR(CDCl₃) δ: 1.13(1H, m), 1.24–1.31(2H, m), 1.44–1.51(2H, m),1.60–1.77(4H, m), 2.03–2.22(5H, m), 2.36(2H, t, J=7.2 Hz), 2.56(1H, s),3.88(1H, m),4.39(2H, s), 5.31–5.45(2H, m), 6.26(1H, d, J=7.2 Hz),6.90–6.94(2H, m), 7.15(1H, dd, J=1.5 and 5.1 Hz), 7.27(1H, d, J=7.5 Hz),7.36 (1H, t, J=7.5 Hz), 7.71(1H, d, J=7.5 Hz), 7.80(1H, s). IR(CHCl₃):3510, 3444, 3423, 2667, 1709, 1649, 1537, 1504 cm⁻¹. [α]_(D)²⁵+76.6±1.2°(c=1.00³, MeOH) Anal. (C₂₃H₃₁NO₃S₂) Calcd.(%): C, 68.12; H,6.33; N, 2.84; S, 12.99. Found(%): C, 67.83; H, 6.45; N, 3.04; S, 13.03.

Compound Number I-179

¹H-NMR(CDCl₃) δ: 1.04(1H, m), 1.18–1.28(2H, m), 1.39–1.47(2H, m),1.56–1.78(4H, m), 1.98–2.18(5H, m), 2.34(2H, t, J=7.2 Hz), 2.50(1H, m),3.8(1H, m), 4.08(2H, s), 5.29–5.41(2H, m), 5.95(1H, d, J=7.2 Hz), 6.53(1H, d, J=3.6 Hz), 7.23–7.41(10H, m). IR(CHCl₃): 3516, 3446, 3427, 1741,1709, 1641, 1543, 1506, 1479, 1456 cm⁻¹. [α]_(D)^(24.5)+57.6±1.0°(c=1.007, MeOH) Anal. (C₃₂H₃₅NO₃S.0.2H₂O) Calcd.(%): C,74.30; H, 6.90; N, 2.71; S, 6.20. Found(%): C, 74.24; H, 6.89; N, 2.88;S, 6.47.

Compound Number I-180

¹H-NMR(CDCl₃) δ: 1.17(1H, m), 1.24–1.35(2H, m), 1.48–1.55(2H, m),1.61–1.79(4H, m), 2.06–2.26(5H, m), 2.37(2H, t, J=7.2 Hz), 2.61(1H, m),3.90 (1H, m), 5.33–5.48(2H, m), 6.44(1H, d, J=7.2 Hz), 7.31(1H, m),7.47–7.65 (5H, m), 7.90(1H, s). IR(CHCl₃): 3516, 3440, 1714, 1655, 1604,1514, 1473, 1446 cm⁻¹. [α]_(D) ²⁵+92.1±1.3°(c=1.001, MeOH) Anal.(C₂₈H₂₉NO₄.0.3H₂O) Calcd.(%): C, 74.91; H, 6.65; N, 3.12. Found(%): C,74.81; H, 6.51; N, 3.29.

Compound Number I-181

¹H-NMR(CDCl₃) δ: 1.04(1H, m), 1.18–1.28(2H, m), 1.41–1.46(2H, m),1.55–1.77(4H, m), 1.99–2.16(5H, m), 2.34(2H, t, J=7.4 Hz), 2.51(1H, s),3.79(3H, s),3.80(1H, m), 4.08(2H, s), 5.29–5.42(2H, m), 5.97(1H, d,J=7.2 Hz), 6.75(1H, d, J=3.9 Hz), 6.85 and 7.15(each 2H, each d, J=8.4Hz), 7.37(1H, d, J=3.9 Hz). IR(CHCl₃): 3518, 3446, 3427, 1741, 1709,1641, 1612, 1543, 1510, 1458 cm⁻¹. [α]_(D) ²⁵+63.6±1.0°(c=1.000, MeOH)Anal. (C₂₇H₃₃NO₄S.0.2H₂O) Calcd.(%): C, 68.88; H, 7.14; N, 2.97; S,6.80. Found(%): C, 68.92; H, 7.02; N, 3.12; S, 6.96.

Compound Number I-182

¹H-NMR(CDCl₃) δ: 1.04(1H, m), 1.18–1.27(2H, m), 1.40–1.45(2H, m),1.59–1.78(4H, m), 1.99–2.14(5H, m), 2.34(2H, t, J=7.4 Hz), 2.51(1H, s),3.80 (1H, m),4.37(2H, s), 5.29–5.41(2H, m), 5.97(1H, d, J=7.2 Hz), 6.82(1H, d, J=3.6 Hz), 7.20(1H, s), 7.34–7.37(3H, m), 7.69(1H, m), 7.86(1H,m). IR (CHCl₃): 3512, 3444 3427, 2669, 1709, 1643, 1543, 1508, 1458,1431 cm⁻¹. [α]_(D) ²⁵+60.7±1.0°(c=1.008, MeOH) Anal.(C₂₈H₃₁NO₃S₂.0.3H₂O) Calcd.(%): C, 67.39; H, 6.38; N, 2.81; S, 12.85.Found(%): C, 67.44; H, 6.30; N, 3.15; S, 12.81.

Compound Number I-183

¹H-NMR(CDCl₃) δ: 1.04(1H, m), 1.18–1.26(2H, m), 1.39–44(2H, m),1.54–1.75(4H, m), 1.99–2.15(5H, m), 2.32(2H, t, J=7.4 Hz), 2.50(1H, s),3.80 (1H, m),4.12(2H, s), 5.28–5.42(2H, m), 6.05(1H, d, J=7.5 Hz), 6.78(1H, d, J=3.9 Hz), 6.82–6.87(2H, m), 7.07–7.14(2H, m), 7.35(1H, d, J=3.9Hz). IR (CHCl₃): 3508, 3444, 3197, 1707, 1635, 1543, 1508, 1456 cm⁻¹.[α]_(D) ²⁵+64.7±1.0°((c=1.004, MeOH) Anal. (C₂₆H₃₁NO₄S.0.2H₂O)Calcd.(%): C, 68.30; H, 6.92; N, 3.06; S, 7.01. Found(%): C, 68.21; H,6.96; N, 3.09; S, 6.93.

Compound Number I-184

¹H-NMR(CDCl₃) δ: 1.15(1H, m), 1.26–1.35(2H, m), 1.47–1.56(2H, m),1.62–1.82(4H, m), 2.05–2.26(5H, m), 2.37(2H, t, J=7.2 Hz), 2.61(1H, m),3.92(1H, m), 3.93(2H, s), 5.32–5.47(2H, m), 6.34(1H, d, J=6.9 Hz),7.31–7.43 (2H, m), 7.53–7.59(2H, m), 7.67(1H, m), 7.5(1H, d, J=6.9 Hz),8.17 (1H, s). IR(CHCl₃): 3514, 3444, 2667, 1709, 1651, 1572, 1516, 1481,1452 cm⁻¹. [α]_(D) ²⁴+81.2±1.2°(c=1.002, MeOH) Anal. (C₂₈H₃₁NO₃.0.2H₂O)Calcd.(%): C, 77.64; H, 7.31; N, 3.23. Found(%): C, 77.59; H, 7.15; N,3.44.

Compound Number I-185

¹H-NMR(CDCl₃) δ: 1.06(1H, m), 1.21–1.28(2H, m), 1.41–1.46(2H, m),1.58–1.78(4H, m), 2.00–2.16(5H, m), 2.35(2H, t, J=7.2 Hz), 2.51(1H, m),3.79 (1H, m), 4.16(2H, s), 5.31–5.40(2H, m), 5.93(1H, d, J=7.8 Hz), 6.80(1H, d, J=3.6 Hz), 7.03–7.12(2H, m), 7.20–7.28(2H, m), 7.35(1H, d, J=3.6Hz). IR (CHCl₃): 3518, 3444, 3427, 1741, 1709, 1643, 1543, 1506, 1456cm⁻¹. [α]_(D) ²⁴+56.2±0.9°(c=1.03, CHCl₃) Anal. (C₂₆H₃₀FNO₃S.0.4H₂O)Calcd.(%): C, 67.48; H, 6.71; N, 3.03; S, 6.93; F, 4.11. Found(%): C,67.49; H, 6.72; N, 3.09; S, 6.93; F, 4.11.

Compound Number I-186

¹H-NMR(CDCl₃) δ: 1.04(1H, m), 1.19–1.29(2H, m), 1.41–1.46(2H, m),1.58–1.82(4H, m), 2.00–2.16(5H, m), 2.34(2H, t, J=7.4 Hz), 2.51(1H, s),3.80(1H, m),4.17(2H, s), 5.08(2H, s), 5.28–5.41(2H, m), 5.90(1H, d,J=7.5 Hz), 6.76(1H, d, J=3.9 Hz), 6.90–6.95(2H, m), 7.18–7.25(2H, m),7.31–7.38 (6H, m). IR(CHCl₃): 3516, 3446, 3427, 1741, 1709, 1641, 1601,1543, 1502, 1454 cm⁻¹. [α]_(D) ²⁴+53.9±0.9°(c=1.005, MeOH) Anal.(C₃₃H₃₇NO₄S) Calcd.(%): C, 72.90; H, 6.86; N, 2.58; S, 5.90. Found(%):C, 72.64; H, 6.92; N, 2.52; S, 5.74.

Compound Number I-187

¹H-NMR(CDCl₃) δ: 1.04(1H, m), 1.18–1.28(2H, m), 1.41–1.46(2H, m),1.57–1.78(4H, m), 1.99–2.15(5H, m), 2.34(2H, t, J=7.4 Hz), 2.51(1H, s),3.80 (1H, m),4.16(2H, s), 4.54–4.57(2H, m), 5.24–5.41(4H, m), 5.94(1H,d, J=7.5 Hz), 6.04(1H, m), 6.79(1H, d, J=3.9 Hz), 6.85–6.93(2H, m),7.15–7.24 (2H, m), 7.34(1H, d, J=3.9 Hz). IR(CHCl₃): 3516, 3446, 3427,1739, 1709, 1641, 1543, 1506, 1477 cm⁻¹. [α]_(D) ²⁴+59.0±1.0°(c=1.007,MeOH) Anal. (C₂₉H₃₅NO₄S.0.2H₂O) Calcd.(%): C, 70.05; H, 7.18; N, 2.82;S, 6.45. Found(%): C, 69.97; H, 7.16; N, 2.80; S, 6.52.

Compound Number I-188

mp.84–85° C.; ¹-NMR(CDCl₃) δ: 1.04(1H, m), 1.18–1.29(2H, m), 1.41–1.46(2H, m), 1.56–1.81(4H, m), 2.00–2.17(5H, m), 2.35(2H, t, J=7.2 Hz), 2.51(1H, s), 3.80(1H, m),4.07(2H, s), 5.05(2H, s), 5.29–5.42(2H, m), 5.93(1H, d, J=7.5 Hz), 6.75(1H, d, J=3.9 Hz), 6.92 and 7.15(each 2H, each d,J=8.7 Hz), 7.31–7.44(6H, m). IR(CHCl₃): 3521, 3446, 3427, 1741, 1709,1643, 1612, 1543, 1510, 1456 cm⁻¹. [α]_(D) ²⁴+56.1±1.0°(c=1.002, MeOH)Anal. (C₃₃H₃₇NO₄S) Calcd.(%): C, 72.90; H, 6.86; N, 2.58; S, 5.90.Found(%): C, 72.78; H, 6.88; N, 2.74; S, 5.84.

Compound Number I-189

¹H-NMR(CDCl₃) δ: 1.04(1H, m), 1.19–1.29(2H, m), 1.41–1.46(2H, m),1.56–1.79(4H, m), 2.00–2.15(5H, m), 2.35(2H, t, J=7.2 Hz), 2.51(1H, s),3.80 (1H, m),4.07(2H, s), 4.51–4.53(2H, m), 5.26–5.44(4H, m), 5.94(1H,d, J=7.5 Hz), 6.05(1H, m), 6.76(1H, d, J=3.9 Hz), 6.87 and 7.14(each 2H,each d, J=8.7 Hz), 7.36(1H, d, J=3.9 Hz). IR(CHCl₃): 3512, 3446, 3427,1741, 1709, 1643, 1612, 1543, 1508, 1458 cm⁻¹. [α]_(D)²⁴+61.6±1.0°(c=1.004, MeOH) Anal. (C₂₉H₃₅NO₄S.0.4H₂O) Calcd.(%): C,69.54; H, 7.20; N, 2.78; S, 6.40. Found(%): C, 69.47; H, 7.22; N, 2.84;S, 6.51.

Compound Number I-190

¹H-NMR(CDCl₃) δ: 1.05(1H, m), 1.18–1.32(2H, m), 1.39–1.48(2H, m),1.54–1.80(4H, m), 1.98–2.20(5H, m), 2.34(2H, t, J=7.2 Hz), 2.51(1H, m),3.81(1H, m), 4.04(2H, s), 5.29–5.42(2H, m), 5.93(1H, d, J=7.5 Hz),6.68–6.78(2H, m), 7.36(1H, d, J=3.6 Hz). IR(CHCl₃): 3517, 3446, 3427,1741, 1709, 1643, 1543, 1504, 1489, 1444, 1250, 1041 cm⁻¹. [α]_(D)²⁴+59.4±1.0°(c=1.0111, MeOH) Anal. (C₂₇H₃₁NO₅S) Calcd.(%): C, 67.34; H,6.49; N, 2.91; S, 6.66. Found(%): C, 67.27; H, 6.45; N, 3.04; S, 6.63.

Compound Number I-191

¹H-NMR(CDCl₃) δ: 1.06(1H, m), 1.18–1.32(2H, m), 1.39–1.48(2H, m),1.54–1.80(4H, m), 1.98–2.20(5H, m), 2.34(2H, t, J=7.5 Hz), 2.51(1H, m),3.81 (1H, m), 4.12(2H, s), 5.30–5.42(2H, m), 6.04(1H, d, J=7.2 Hz), 6.77(1H, d, J=3.6 Hz), 6.89–7.04(3H, m), 7.28(1H, m), 7.38(1H, d, J=3.6 Hz).IR(CHCl₃): 3518, 3446, 3427, 1739, 1709, 1643, 1545, 1506 cm⁻¹. [α]_(D)²⁵+62.6±1.0°(c=1.009, MeOH) Anal. (C₂₆H₃₀FNO₃S) Calcd.(%): C, 68.54; H,6.64; N, 3.07; S, 7.04; F, 4.17. Found(%): C, 68.25; H, 6.37; N, 3.19;S, 7.12; F, 4.12.

Compound Number I-192

¹H-NMR(CDCl₃), : 1.06(1H, m), 1.18–1.32(2H, m), 1.40–1.48(2H, m),1.54–1.80(4H, m), 1.98–2.20(5H, m), 2.35(2H, t, J=7.5 Hz), 2.52(1H, m),3.81(1H, m), 4.19(2H, s), 5.30–5.42(2H, m), 5.99(1H, d, J=7.2 Hz), 6.78and 7.37(each 1H, each d, each J=3.6 Hz), 7.40–7.54(4H, m). IR(CHCl₃):3516, 3446, 3427, 1740, 1709, 1643, 1545, 1506, 1450, 1330, 1167, 1130,1074 cm⁻¹. [α]_(D) ²⁵+55.4±0.9°(c=1.029, MeOH) Anal. (C₂₇H₃₀F₃NO₃S)Calcd.(%): C, 64.14; H, 5.98; N, 2.77; S, 6.34; F, 11.27. Found(%): C,63.95; H, 5.99; N, 2.90; S, 6.36; F, 10.98.

Compound Number I-193

¹H-NMR(CDCl₃) δ: 1.05(1H, m), 1.24–1.28(2H, m), 1.42–1.46(2H, m),1.58–1.79(4H, m), 2.01–2.21(5H, m), 2.35(2H, t, J=7.2 Hz), 2.51(1H, m),3.80 (1H, m), 4.26(2H, s), 5.33–5.38(2H, m), 5.94(1H, (c, J=7.2 Hz),6.79 (1H, d, J=3.9 Hz), 7.21–7.28(3H, m), 7.35–7.40(2H, m). IR(CHCl₃):3518, 3446, 3427, 1743, 1709, 1643, 1543, 1506 cm⁻¹. [α]_(D)²⁵+55.5±0.9°(c=1.06, CHCl₃) Anal. (C₂₆H₃₀ClNO₃S.0.3H₂O) Calcd.(%): C,65.41; H, 6.46; N, 2.93; S, 6.72; Cl, 7.43. Found(%): C, 65.41; H, 6.40;N, 3.08; S, 6.75; Cl, 7.31.

Compound Number I-194

¹H-NMR(CDCl₃) δ: 1.04(1H, m), 1.18–1.28(2H, m), 1.39–1.46(2H, m),1.56–1.78 (4H, m), 1.98–2.16(5H, m), 2.30(6H, s), 2.34(2H, t, J=7.2 Hz),2.50 (1H, m), 3.80(1H, m), 4.16(2H, s), 5.28–5.41(2H, m), 5.93(1H, d,J=6.9 Hz), 6.78(1H, d, J=3.9 Hz), 7.03–7.14(3H, m), 7.77(1H, d, J=3.9Hz). IR (CHCl₃): 3516, 3446, 3427, 2669, 1709, 1641, 1543, 1506, 1456cm⁻¹. [α]_(D) ²⁴+66.6±1.0°(c=1.009, MeOH) Anal. (C₂₈H₃₅NO₃S.0.2H₂O)Calcd.(%): C, 71.67; H, 7.60; N, 2.98; S, 6.83. Found(%): C, 71.71; H,7.54; N, 3.15; S, 6.81.

Compound Number I-195

¹H-NMR(CDCl₃) δ: 1.05(1H, m), 1.22–1.28(2H, m), 1.42–1.47(2H, m),1.59–1.78(4H, m), 2.01–2.17(5H, m), 2.35(2H, t, J=7.2 Hz), 2.50(1H, m),3.82(1H, m), 4.32(2H, s), 5.35–5.37(2H, m), 5.94(1H, d, J=6.9 Hz), 6.76(1H, d, J=3.9 Hz), 7.33–7.39(3H, m), 7.50 (1H, m), 7.69(1H, d, J=3.9Hz). IR (CHCl₃): 3316, 3446, 3427, 1743, 1709, 1643, 1543, 1506, 1456,1163, 1126 cm⁻¹. [α]_(D) ²⁵+54.5±1.0°(c=1.00, CHCl₃) Anal.(C₂₇H₃₀F₃NO₃S.0.2H₂O) Calcd.(%): C, 63.93; H, 6.02; N, 2.75; S, 6.30.Found(%): C, 63.92; H, 5.85; N, 2.94; S, 6.38.

Compound Number I-196

¹H-NMR(CDCl₃) δ: 1.05(1H, m), 1.22–1.28(2H, m), 1.42–1.46.(2H, m),1.58–1.80 (4H, m), 2.01–2.21(5H, m), 2.35(2H, t, J=7.2 Hz), 2.52(1H, m),3.81 (1H, m), 3.88(3H, s), 4.06(2H, s), 5.33–5.38(2H, m), 5.94(1H, d,J=10.2 Hz), 6.70(1H, d, J=3.6 Hz), 6.87–6.97(3H, m), 7.36(1, d, J=3.6Hz). IR (CHCl₃): 3517, 3446, 3427, 2673, 1741, 1709, 1643, 1543, 1516,1274 1030 cm⁻¹. [α]_(D) ²⁵+54.2±0.9°(c=1.00, CHCl₃) Anal.(C₂₇H₃₂FNO₄S.0.3H₂O) Calcd.(%): C, 66.04; H, 6.69; N, 2.85; S, 6.53; F,3.87. Found(%): C, 66.16; H, 6.61; N, 2.82; S, 6.34; F, 3.66.

Compound Number I-197

¹H-NMR(CDCl₃) δ: 1.05(1H, m), 1.18–1.27(2H, m), 1.41–1.45(2H, m),1.56–1.77(4H, m), 1.98–2.13(5H, m), 2.34(2H, t, J=7.5 Hz), 2.50(1H, s),3.21 (2H, t, J=8.7 Hz), 3.80(1H, m), 4.07(2H, s), 4.57(2H, t, J=8.7 Hz),5.29–5.41 (2H, m), 6.00(1H, d, J=7.5 Hz), 6.79(1H, d, J=3.6 Hz),6.79(1H, dd, J=7.2 and 7.5 Hz), 6.95(1H, d, J=7.5 Hz), 7.09(1H, d, J=7.2Hz), 7.36(1H, d, J=3.6 Hz). IR(CHCl₃): 3514, 3446, 3427, 2669,.1739,1709, 1641, 1543, 1506, 1477, 1456, 1441 cm⁻¹. [α]_(D)²⁵+61.1±1.0°(c=1.004, MeOH) Anal. (C₂₈H₃₃NO₄S.0.2H₂O) Calcd.(%): C,69.60; H, 6.97; N, 2.90; S, 6.63. Found(%): C, 69.68; H, 6.89; N, 3.19;S, 6.65.

Compound Number I-198

¹H-NMR(CDCl₃) δ: 1.04(1H, m), 1.18–1.27(2H, m), 1.40–1.46(2H, m),1.56–1.76(4H, m), 1.98–2.13(5H, m), 2.33(2H, t, J=7.5 Hz), 2.50(1H, s),3.21(2H, t, J=8.7 Hz), 3.80(1H, m), 4.24(2H, s), 5.28–5.40(2H, m),5.97(1H, d, J=7.2 Hz), 6.79(1H, d, J=3.6 Hz), 7.22(1H, dd, J=1.2 and 8.1Hz), 7.29 (1H, d, J=5.4 Hz), 7.38(1H, d,J=3.6 Hz), 7.44(1H, d, J=5.4Hz), 7.68(1H, d, J=1.2 Hz), 7.81(1H, d, J=8.1 Hz). IR(CHCl₃): 3516,3446, 3427, 1741, 1709, 1643, 1543, 1506, 1547 cm⁻¹. [α]_(D)²⁵+62.0±1.0°(c=1.000, MeOH) Anal. (C₂₈H₃₁NO₃S₂.0.2H₂O) Calcd.(%): C,67.63; H, 6.36; N, 2.82; S, 12.90. Found(%): C, 67.55; H, 6.28; N, 2.97;S, 12.90.

Compound Number I-199

¹H-NMR(CDCl₃) δ: 1.04(1H, m), 1.17–1.27(2H, m), 1.40–1.45(2H, m),1.54–1.77(4H, m), 1.98–2.15(5H, m), 2.34(2H, t, J=7.2 Hz), 2.51(1H, s),3.80 (1H, m),4.25(2H, s), 5.28–5.41(2H, m), 5.97(1H, d, J=7.2 Hz),6.79(1H, d, J=3.9 Hz), 7.24(1H, dd, J=1.5 and 8.1 Hz), 7.30(1H, d, J=5.4Hz), 7.38(1H, d, J=3.6 Hz), 7.41(1H, d, J=5.4 Hz), 7.73(1H, m), 7.76(1H,d, J=8.1 Hz). IR(CHCl₃): 3516, 3447, 3427, 1741, 1709, 1643, 1543, 1506,1458 cm⁻¹. [α]_(D) ²⁵+62.1±1.0°(c=1.008, MeOH) Anal.(C₂₈H₃₁NO₃S₂.0.3H₂O) Calcd.(%): C, 67.39; H, 6.38; N, 2.81; S, 12.85.Found(%): C, 67.42; H, 6.29; N, 2.99; S, 12.94.

Compound Number I-200

¹H-NMR(CDCl₃) δ: 1.03(1H, m), 1.16–1.22(2H, m), 1.39–1.44(2H, m),1.53–1.76 (4H, m), 1.97–2.14(5H, m), 2.33(2H, t, J=7.5 Hz), 2.49(1H, s),3.79 (1H, m),4.39(2H, s), 5.28–5.40(2H, m), 5.98(1H, d, J=7.5 Hz),6.86(1H, d, J=3.9 Hz), 7.21(1H, d, J=6.9 Hz), 7.35(1H, dd, J=6.9 and 8.1Hz), 7.36(1H, d, J=5.4 Hz), 7.36(1H, d, J=3.9 Hz), 7.42(1H, d, J=5.4Hz), 7.74(1H, d, J=8.1 H). IR(CHCl₃): 3516, 3446, 3427, 1739, 1709,1643, 1543, 1506, 1458 cm⁻¹. [α]_(D) ²⁵+58.4±1.0°(c=1.003, MeOH) Anal.(C₂₈H₃₁NO₃S₂.0.2H₂O) Calcd.(%): C, 67.63; H, 6.36; N, 2.82; S, 12.90.Found(%): C, 67.62; H, 6.27; N, 3.09; S, 12.92.

Compound Number I-201

¹H-NMR(CDCl₃+CD₃OD) δ: 1.08(1H, m), 1.22–1.28(2H, m), 1.41–1.46(2H, m),1.55–1.71(4H, m), 2.01–2.10(5H, m), 2.29(2H, t, J=7.4 Hz), 2.51(1H, s),3.77(1H, m), 4.29(2H, s), 5.34–5.40(2H, m), 6.80(1H, d, J=3.9 Hz),6.93(1H, dd, J=1.8 and 8.7 Hz), 7.10(1H, d, J=1.8 Hz), 7.22(1H, s),7.36(1H, d, J=3.9 Hz), 7.65(1H, d, J=8.7 Hz). IR(CHCl₃): 3508, 3423,3236, 1709, 1633, 1601, 1545, 1510, 1441 cm⁻¹. [α]_(D)²⁵+57.5±1.0°(c=1.006, MeOH) Anal. (C₂₈H₃₁NO₄S₂.0.2H₂O) Calcd.(%): C,64.84; H, 6.21; N, 2.70; S, 12.36. Found(%): C, 67.57; H, 6.20; N, 2.93;S, 12.38.

Compound Number I-202

¹H-NMR(CDCl₃) δ: 1.05(1H, m), 1.24–1.28(2H, m), 1.41–1.48(2H, m),1.58–1.79(4H, m), 2.02–2.22(5H, m), 2.33(2H, t, J=7.5 Hz), 2.51(1H, m),3.78 (1H, m), 4.25(2H, s), 4.70(2H, s), 5.31–5.42(2H, m), 6.00(1H, d,J=7.2 Hz), 6.74(1H, d, J=3.6 Hz), 7.24–7.42(5H, m). IR(CHCl₃): 3518,3444, 3427, 1709, 1643, 1543, 1506, 1456 cm⁻¹. [α]_(D)²⁶+51.9±0.9°(c=1.04, CHCl₃) Anal. (C₂₇H₃₃FNO₄S.0.7H₂O) Calcd.(%): C,67.53; H, 7.22; N, 2.92; S, 6.02. Found(%): C, 67.92; H, 7.13; N, 2.88;S, 6.11.

Compound Number I-203

¹H-NMR(CDCl₃) δ: 1.02(1H, m), 1.22–1.28(2H, m), 1.40–1.42(2H, m),1.57–1.72(4H, m), 1.82–1.85(4H, m), 2.01–2.13(5H, m), 2.27(2H, t, J=7.5Hz), 2.49(1H, m), 2.71–2.73(4H, m), 3.67(1H, d, J=13.2 Hz), 3.76 (1H,m),3.83(1H, d, J=13.2 Hz), 4.26(1H, d, J=16.5 Hz), 4.34(1H, d, J=16.5 Hz),5.33–5.45(2H, m), 6.04(1H, d, J=7.2 Hz), 6.70(1H, d, J=3.6 Hz),7.16–7.33 (4H, m), 7.43((1H, d, J=3.6 Hz). IR(CHCl₃): 3518, 3446, 3424,2472, 1707, 1643, 1545, 1506, 1456 cm⁻¹. [α]_(D) ²⁶+41.9.±0.8°(c=1.03,CHCl₃) Anal. (C₃₁H₄₀N₂O₃S.0.6H₂O) Calcd.(%): C, 70.05; H, 7.81; N, 5.27;S, 6.03. Found(%): C, 70.01; H, 7.81; N, 5.18; S, 5.86.

Compound Number I-204

¹H-NMR(CDCl₃) δ: 1.06(1H, m), 1.22–1.29(2H, m), 1.41–1.46(2H, m),1.58–1.72(4H, m), 2.03–2.17(5H, m), 2.31(2H, t, J=7.2 Hz), 2.51(1H, m),2.60 (6H, s), 3.79(1H, m), 3.94(1H, d, J=13.2 Hz), 3.99(1H, d, J=13.2Hz), 4.39 (2H,s), 5.30–5.44(2H, m), 6.01(1H, d, J=7.2 Hz), 6.72(1H, d,J=3.9 Hz), 7.26–7.40(4H, m), 7.56(1H, d, J=7.2 Hz). IR(CHCl₃): 3519,3444, 3425, 2455, 1753, 1712, 1643, 1545, 1508, 1458 cm⁻¹. [α]_(D)²⁶+41.2±0.8°(c=1.02, CHCl₃) Anal. (C₂₉H₃₈N₂O₃S.1.7H₂0.2CHCl₃) Calcd.(%):C, 63.86; H, 7.63; N, 5.10; S, 5.84; Cl, 3.87. Found(%): C, 63.88; H,7.51; N, 4.94; S, 5.63; Cl, 4.22.

Compound Number I-205

¹H-NMR(CDCl₃) δ: 1.14(1H, m), 1.24–1.36(2H, m), 1.45–1.54(2H, m),1.60–1.79(4H, m), 2.03–2.26(5H, m), 2.36(2H, t, J=7.5 Hz), 2.58(1H, m),3.19–3.26(4H, m), 3.89(1H, m), 5.32–5.45(2H, m), 6.33(1H, d, J=6.3 Hz),7.24(1H, d, J=7.2 Hz), 7.34 and 7.46(each 1H, each m), 7.61(1H, dd,J=1.5 and 8.4 Hz), 7.68(1H, d, J=1.5 Hz), 7.98–8.04(2H, m). IR(CHCl₃):3518, 3444, 2667, 1709, 1649, 1597, 1514, 1483, 1450, 1294 cm⁻¹. [α]_(D)²⁵+78.7±1.2°(c=1.003, MeOH) Anal. (C₃₀H₃₃NO₄) Calcd.(%): C, 75.54; H,7.10; N, 2.94. Found(%): C, 75.62; H, 7.05; N, 2.94.

Compound Number I-206

¹H-NMR(CDCl₃₃) δ: 1.10(1H, m), 1.22–1.36(2H, m), 1.40–1.52(2H, m),1.56–1.81(4H, m), 2.00–2.24(5H, m), 2.35(2H, t, J=7.2 Hz), 2.50(1H, m),3.84 (1H, m), 3.99(2H, s), 5.30–5.43(2H, m), 6.05(1H, d, J=3.3 Hz),6.29(1H, d, J=7.8 Hz), 6.99–7.05(3H, m), 7.17–7.22(2H, m). IR(CHCl₃):3512, 3435, 1739, 1709, 1653, 1606, 1549, 1510 cm⁻¹. [α]_(D)²⁶+71.0±1.1°(c=1.005, MeOH) Anal. (C₂₆H₃₀FNO₄O) Calcd.(%): C, 71.05; H,6.88; N, 3.19; F, 4.32. Found(%): C, 70.78; H, 6.97; N, 3.30; F, 4.27.

Compound Number I-207

¹H-NMR(CDCl₃) δ: 1.10(1H, m), 1.22–1.34(2H, m), 1.40–1.50(2H, m),1.56–1.81(4H, m), 2.00–2.24(5H, m), 2.35(2H, t, J=7.2 Hz), 2.50(1H, m),3.84 (1H, m), 4.02(2H, s), 5.30–5.43(2H, m), 6.07(1H, d, J=3.3 Hz),6.30(1H, d, J=7.5 Hz), 7.02(1H, d, J=3.3 Hz), 7.22–7.36(5H, m).IR(CHCl₃): 3516, 3435, 2669, 1709, 1651, 1606, 1547, 1498 cm⁻¹. [α]_(D)²⁴+76.5±1.2°(c=1.005, MeOH) Anal. (C₂₆H₃₁FNO₄.0.1H₂O) Calcd.(%): C,73.77; H, 7.43; N, 3.31. Found(%): C, 73.63; H, 7.27; N, 3.42.

Compound Number I-208

¹H-NMR(CDCl₃) δ: 1.04(1H, m), 1.16–1.26(2H, m), 1.39–1.44(2H, m),1.55–1.76(4H, m), 1.98–2.18(5H, m), 2.33(2H, t, J=7.2 Hz), 2.50(1H, s),3.79 (1H, m),4.42(2H, s), 5.28–5.40(2H, m), 5.98(1H, d, J=6.9 Hz),6.78(1H, d, J=2.1 Hz), 6.84(1H, d, J=3.6 Hz), 7.12–7.21(2H, m), 7.36(1H,d, J=3.6 Hz), 7.50(1H, dd, J=1.5 and 7.5 Hz), 7.63(1H, d, J=2.1 Hz).IR(CHCl₃): 3516, 3446, 3427, 2665, 1741, 1709, 1643, 1523, 1506, 1458,1427 cm⁻¹. [α]_(D) ²⁵+63.4±1.0°(c=1.006, MeOH) Anal. (C₂₈H₃₁NO₄S.0.2H₂O)Calcd.(%): C, 69.89; H, 6.58; N, 2.91; S, 6.66. Found(%): C, 69.68; H,6.48; N, 3.10; S, 6.62.

Compound Number I-209

¹H-NMR(CDCl₃) δ: 1.07(1H, m), 1.22–1.29(2H, m), 1.42–1.47(2H, m),1.59–1.82(4H, m), 2.01–2.20(5H, m), 2.35(2H, t, J=7.2 Hz), 2.52(1H, m),2.94 (3H,s), 3.81(1H, m), 4.19(2H, s), 4.44(2H, s), 5.31–5.38(2H, m),5.35 (1H,d, J=7.2 Hz), 6.63–6.72(4H, m), 7.16–7.25(6H, m), 7.36(1H, d,J=3.6 Hz). IR (CHCl₃): 3514, 3444, 3427, 1741, 1709, 1643, 1599, 1543,1506, 1456 cm⁻¹. [α]_(D) ²⁶+50.8±0.9°(c=1.04, CHCl₃) Anal.(C₃₄H₄₀N₂O₃S.0.7H₂O) Calcd.(%): C, 71.72; H, 7.33; N, 4.92; S, 5.63.Found(%): C, 71.81; H, 7.29; N, 4.81; S, 5.54.

Compound Number I-210

¹H-NMR (CHCl₃) δ: 1.14–1.68(11H, m), 1.91–2.16(9H, m), 2.21(2H, t, J=7.2Hz), 2.57(1H, m), 2.98(1H, m), 3.71(1H, m), 3.89(2H, s), 4.28(1H, d,J=16.5 Hz), 4.30(1H, d, J=16.5 Hz), 5.28–5.50(3H, m), 6.56(1H, m),6.75(1H, m), 7.20–7.33 (2H, m), 7.49–7.55(2H, m). IR(CHCl₃): 3518, 3425,1753, 1711, 1641, 1545, 1508, 1456 cm⁻¹. [α]_(D) ²⁶+35.6±0.7°(c=1.03,CHCl₃)

Compound Number I-211

¹H-NMR(CDCl₃) δ: 1.04(1H, m), 1.17–1.28(2H, m), 1.39–1.46(2H, m),1.54–1.78(4H, m), 1.98–2.19(5H, m), 2.33(2H, t, J=7.2 Hz), 2.51(1H, m),3.80(1H, m), 4.29(2H, s), 5.28–5.40(2H, m), 5.95(1H, d, J=7.2 Hz),6.82(1H, d, J=3.6 Hz), 7.23(1H, dd, J=1.5 and 8.1 Hz), 7.30–7.47(4H, m),7.55(1H, d, J=8.1 Hz), 7.89(1H, d, J=7.8 Hz), 7.93(1H, dd, J=1.5 and 7.8Hz). IR (CHCl₃): 3510, 3446, 3427, 2671, 1739, 1709, 1641, 1545, 1506,1458, 1427 cm⁻¹. [α]_(D) ²⁴+60.2±1.0°(c=1.006, MeOH) Anal.(C₃₂H₃₃NO₄S.0.2H₂O) Calcd.(%): C, 72.34; H, 6.34; N, 2.64; S, 6.04.Found(%): C, 72.28; H, 6.25; N, 2.72; S, 5.93.

Compound Number I-212

¹H-NMR(CDCl₃) δ: 1.05(1H, m), 1.18–1.30(2H, m), 1.38–1.47(2H, m),1.54–1.80(4H, m), 1.98–2.20(5H, m), 2.34(2H, t, J=7.5 Hz), 2.51(1H, m),3.78 (3H, s), 3.80(1H, m), 3.86(3H, s), 4.15(2H, s), 5.29–5.42(2H, m),5.93(1H, d, J=7.5 Hz), 6.78–6.85(3H, m), 7.01(1H, t, J=8.1 Hz), 7.36(1H,d, J=3.9 Hz). IR(CHCl₃): 3516, 3446, 3425, 2667, 1739, 1709, 1641, 1543,1506, 1481, 1273, 1076 cm⁻¹. [α]_(D) ²⁵+60.8±1.0°(c=1.002, MeOH) Anal.(C₂₈H₃₅NO₅S.0.1H₂O) Calcd.(%): C, 67.33; H, 7.10; N, 2.80; S, 6.42.Found(%): C, 67.21; H, 7.08; N, 2.92; S, 6.45.

Compound Number I-213

¹H-NMR(CDCl₃) δ: 1.08(1H, m), 1.19–1.30(2H, m), 1.42–1.47(2H, m),1.58–1.78(4H, m), 2.01–2.16(5H, m), 2.38(2H, t, J=7.2 Hz), 2.39(3H, s),2.53 (1H, s),3.82(1H, m), 4.15(2H, s), 5.31–5.44(2H, m), 5.87(1H, s),6.05(1H, d, J=7.2 Hz), 6.86(1H, d, J=3.9 Hz), 7.38(1H, d, J=3.9 Hz).IR(CHCl₃): 3516, 3444, 3427, 2669, 1709, 1643, 1608, 1545, 1508, 1456cm⁻¹. [α]_(D) ²⁵+64.3±1.0°(c=1.012, MeOH) Anal. (C₂₄H₃₀N₂O₄S.0.2H₂O)Calcd.(%): C, 64.61; H, 6.87; N, 6.28; S, 7.19. Found(%): C, 64.70; H,6.84; N, 6.34; S, 7.27.

Compound Number I-214

¹H-NMR(CDCl₃) δ: 1.06(1H, m), 1.19–1.28(2H, m), 1.41–1.46(2H, m),1.58–1.79(4H, m), 2.00–2.15(5H, m), 2.33–2.37(5H, m), 2.51(1H, s),3.81–3.82 (4H,m), 4.08(2H, s), 5.29–5.42(2H, m), 5.93(1H, d, J=6.9 Hz),6.70(1H, s), 6.72(1H, d, J=7.8 Hz), 6.77(1H, d, J=3.6 Hz), 7.04(1H, d,J=7.8 Hz), 7.34 (1H, d, J=3.6 Hz). IR(CHCl₃): 3516, 3446, 3427, 2669,1741, 1709, 1641, 1614, 1583, 1506, 1458 cm⁻¹. [α]_(D)²⁵+58.9±1.0°(c=1.012, MeOH) Anal. (C₂₈H₃₅N₄S.0.2H₂O) Calcd.(%): C,69.31; H, 7.35; N, 2.89; S, 6.61. Found(%): C, 69.21; H, 7.35; N, 3.03;S, 6.65.

Compound Number I-215

mp.128–129° C.; ¹H-NMR(CDCl₃) δ: 1.05 (1H, m), 1.19–1.28 (2H, m),1.41–1.46 (2H, m), 1.56–1.79(4H, m), 2.00–2.15(5H, m), 2.34(2H, t, J=7.2Hz), 2.51(1H, s), 3.80(1H, m), 3.84(3H, s), 4.33(2H, s), 5.29–5.42 (2H,m), 5.94(1H, d, J=6.9 Hz), 6.83(1H, d, J=3.6 Hz), 7.01(1H, dd, J=2.7 and9.0 Hz), 7.11(1H, d, J=2.7 Hz), 7.21(1H, s), 7.36(1H, d, J=3.6 Hz), 7.72(1H, d, J=9.0 Hz). IR(CHCl₃): 3516, 3446, 3427, 1739, 1709, 1643, 1601,1543, 1506, 1458, 1427 cm⁻¹. [α]_(D) ²⁵+55.7±1.0°(c=1.008, MeOH) Anal.(C₂₉H₃₃NO₄S₂) Calcd.(%): C, 66.51; H, 6.35; N, 2.67; S, 12.25. Found(%):C, 66.41; H, 6.30; N, 2.96; S, 12.15.

Compound Number I-216

¹H-NMR(CDCl₃) δ: 1.04(1H, m), 1.16–1.29(2H, m), 1.39–1.46(2H, m),1.55–1.79 (4H, m), 1.98–2.19(5H, m), 2.34(2H, t, J=7.2 Hz), 2.51(1H, m),3.80 (1H, m), 3.87 and 4.20(each 2H, each s), 5.28–5.40(2H, m), 5.93(1H,d, J=8.1 Hz), 6.81(1H, d, J=3.9 Hz), 7.24–7.39(5H, m), 7.53(1H, d, J=7.2Hz), 7.71–7.77(2H, m). IR(CHCl₃): 3516, 3446, 3427, 1739, 1709, 1643,1543, 1506, 1456 cm⁻¹. [α]_(D) ²⁵+56.7±1.0°(c=1.000, MeOH) Anal.(C₃₃H₃₅NO₃S.0.1H₂O) Calcd.(%): C, 75.14; H, 6.73; N, 2.66; S, 6.08.Found(%): C, 75.14; H, 6.80; N, 2.74; S, 5.83.

Compound Number I-217

¹H-NMR(CDCl₃) δ: 1.07(1H, m), 1.19–1.32(2H, m), 1.40–1.48(2H, m),1.56–1.78 (4H, m), 2.00–2.21(5H, m), 2.34(2H, t, J=7.5 Hz), 2.54(1H, m),3.13–3.24 (4H, m), 3.85(1H, m), 4.13(2H, s), 5.28–5.42(2H, m), 6.17(1H,d, J=7.2 Hz), 7.06–7.17(4H, m), 7.22(1H, d, J=7.8 Hz), 7.44(1H, dd,J=1.8 and 7.8 Hz), 7.53(1H, d, J=1.8 Hz). IR(CHCl₃): 3518, 3446, 1739,1709, 1651, 1570, 1518, 1491, 1456 cm⁻¹. [α]_(D) ²⁵+73.3±1.1°(c=1.000,MeOH) Anal. (C₃₀H₃₅NO₃.0.2H₂O) Calcd.(%): C, 78.13; H, 7.44; N, 3.04.Found(%): C, 78.25; H, 7.76; N, 3.29.

Compound Number I-218

¹H-NMR(CDCl₃) δ: 1.05(1H, m), 1.18–1.30(2H, m), 1.39–1.48(2H, m),1.54–1.81(4H, m), 1.98–2.20(5H, m), 2.34(2H, t, J=7.2 Hz), 2.51(1H, m),3.80(1H, m), 3.82, 3.85 and 3.87(each 3H, each s), 4.07(2H, s),5.29–5.42 (2H, m), 5.94(1H, d, J=7.5 Hz), 6.62(1H, d, J=8.7 Hz),6.76(1H, d, J=3.6 Hz), 6.85(11H, d, J=8.7 Hz), 7.35(1H, d, J=3.6 Hz).IR(CHCl₃): 3514, 3446, 3427, 1739, 1709, 1641, 1603, 1543, 1495, 1468,1277, 1259, 1097 cm⁻¹. [α]_(D) ²⁶+54.8±1.0°(c=1.013, MeOH) Anal.(C₂₉H₃₇NO₆S.0.2H₂O) Calcd.(%): C, 65.56; H, 7.10; N, 2.64; S, 6.04.Found(%): C, 65.54; H, 6.96; N, 2.74; S, 5.98.

Compound Number I-219

¹H-NMR(CDCl₃) δ: 1.05(1H, m), 1.18–1.30(2H, m), 1.39–1.48(2H, m),1.54–1.81(4H, m), 1.98–2.20(5H, m), 2.34(2H, t, J=7.2 Hz), 2.51(1H, m),3.80 (1H, m), 3.82, 3.85 and 3.87(each 3H, each s), 4.07(2H, s),5.29–5.42 (2H, m), 5.94(1H, d, J=7.5 Hz), 6.62(1H, d, J=8.7 Hz),6.76(1H, d, J=3.6 Hz), 6.85(1H, d, J=8.7 Hz), 7.35(1H, d, J=3.6 Hz).IR(CHCl₃): 3514, 3446, 3427, 1739, 1709, 1641, 1603, 1543, 1495, 1468,1277, 1259, 1097 cm⁻¹. [α]_(D) ²⁶+54.8±1.0°(c=1.013, MeOH) Anal.(C₂₉H₃₇NO₆S.0.2H₂O) Calcd.(%): C, 65.56; H, 7.10; N, 2.64; S, 6.04.Found(%): C, 65.54; H, 6.96; N, 2.74; S, 5.98.

Compound Number I-220

mp.131–133° C.; ¹H-NMR(CDCl₃) δ: 1.06(1H, m), 1.18–1.31(2H, m),1.40–1.48 (2H, m), 1.56–1.82(4H, m), 2.00–2.21(5H, m), 2.35(2H, t, J=7.5Hz), 2.52 (1H, m), 3.82(1H, m), 3.83(3H, s), 3.84(6H, s), 4.07(2H, s),5.30–5.42 (2H, m), 5.95(1H, d, J=7.5 Hz), 6.45(2H, s), 6.79(1H, d, J=3.6Hz), 7.36(1H, d, J=3.6 Hz). IR(CHCl₃): 3516, 3446, 3427, 1739, 1709,1643, 1593, 1543, 1506, 1462, 1421, 1331, 1240, 1130 cm⁻¹. [α]_(D)²⁴+57.5±1.0°(c=1.007, MeOH) Anal. (C₂₉H₃₇NO₆S) Calcd.(%): C, 66.01; H,7.07; N, 2.65; S, 6.08. Found(%): C, 65.84; H, 6.93; N, 2.71; S, 6.06.

Compound Number I-221

¹H-NMR(CDCl₃) δ: 1.05(1H, m), 1.17–1.30(2H, m), 1.39–1.48(2H, m),1.54–1.80(4H, m), 1.98–2.20(5H, m), 2.34(2H, t, J=7.5 Hz), 2.51(1H, m),3.81 (1H, m), 4.08(2H, s), 5.29–5.42(2H, m), 5.95(2H, s), 5.98(1H, d,J=7.5 Hz), 6.68–6.80(4H, m), 7.35(1H, d, J=3.9 Hz). IR(CHCl₃): 3516,3446, 3427, 1741, 1709, 1641, 1543, 1504, 1460, 1252, 1063 cm⁻¹. [α]_(D)²⁴+62.7±1.0°(c=1.006, MeOH) Anal. (C₂₇H₃₁NO₅S) Calcd.(%): C, 67.34; H,6.49; N, 2.91; S, 6.66. Found(%): C, 67.12; H, 6.37; N, 2.98; S, 6.55.

Compound Number I-222

¹H-NMR(CDCl₃) δ: 1.08(1H, m), 1.24–1.28(2H, m), 1.41–1.45(2H, m),1.56–1.78(4H, m), 1.97–2.20(5H, m), 2.14(3H, s), 2.33(2H, t, J=7.2 Hz),2.51 (1H, m), 3.77(1H, m), 4.06(2H, s), 5.28–5.42(2H, m), 6.16(1H, d,J=7.2 Hz), 6.74 (1H, d, J=3.6 Hz), 6.96(1H, d, J=7.5 Hz), 7.24(1H, t,J=8.7 Hz), 7.35–7.38 (3H, m), 7.74(1H, br s). IR(KBr): 3309, 1707, 1672,1614, 1547, 1523, 1489, 1441, 1371, 1319 cm⁻¹. [α]_(D)²⁶+57.7±1.0°(c=1.012, MeOH) Anal. (C₂₈H₃₄N₂O₄S.0.4H₂O) Calcd.(%): C,67.01; H, 6.99; N, 5.58; S, 6.39. Found(%): C, 66.98; H, 6.72, N, 5.47;S, 6.27.

Compound Number I-223

¹H-NMR(CDCl₃) δ: 1.05(1H, m), 1.22–1.28(2H, m), 1.42–1.46(2H, m),1.55–1.75(4H, m), 2.02–2.22(5H, m), 2.34(2H, t, J=7.5 Hz), 2.51(1H, m),2.99 (3H, s), 3.81(1H, m), 4.11(2H, s), 5.29–5.45(2H, m), 6.04(1H, d,J=7.2 Hz), 6.78 (1H, d, J=3.6 Hz), 7.04–7.06(2H, m), 7.16(1H, m),7.25(1H, br s), 7.29(1H, t, J=7.8 Hz), 7.36 (1H, d, J=3.6 Hz). IR(CHCl₃): 3512, 3444, 3427, 3371, 1709, 1639, 1608, 1545, 1508, 1475,1458, 1389, 1335, 1151 cm⁻¹. [α]_(D) ²⁴+55.0±1.0°(c=1.003, MeOH) Anal.(C₂₇H₃₄N₂O₅S₂.0.2H₂O) Calcd.(%): C, 60.69; H, 6.49; N, 5.24; S, 12.00.Found(%): C, 60.70; H, 6.44; N, 5.15; S, 11.56.

Compound Number I-224

¹H-NMR(CDCl₃) δ: 1.07(1H, m), 1.22–1.28(2H, m), 1.42–1.53(2H, m),1.57–1.74(4H, m), 2.00–2.24(5H, m), 2.35(2H, t, J=7.2 Hz), 2.52(1H, m),3.81 (1H, m), 4.33(2H, s), 5.29–5.42(2H, m), 5.98(1H, d, J=7.8 Hz),6.86, 6.88 and 7.14 (each 1H, each d, each J=3.6 Hz), 7.22–7.37(4H, m),7.53–7.56(2H, m).

Compound Number I-225

¹H-NMR (CDCl₃) δ: 1.05(1H, m), 1.17–1.30(2H, m), 1.39–1.48(2H, m),1.54–1.81(4H, m), 1.98–2.20(5H, m), 2.35(2H, t, J=7.5 Hz), 2.51(1H, m),3.81 (1H, m), 4.08(2H, s), 4.23–4.30(4H, m), 5.29–5.42(2H, m), 5.95(1H,d, J=7.2 Hz), 6.71–6.80(4H, m), 7.34(1H, d, J=3.6 Hz). IR(CHCl₃): 3514,3446, 3427, 1739, 1709, 1641, 1603, 1543, 1506, 1475, 1456, 1284, 1090cm⁻¹. [α]_(D) ^(24.5)+58.9±1.0°(c=1.013, MeOH) Anal. (C₂₈H₃₃NO₅S)Calcd.(%): C, 67.85; H, 6.71; N, 2.83; S, 6.47. Found(%): C, 68.01; H,6.72; N, 2.97; S, 6.50.

Compound Number I-226

¹H-NMR(CDCl₃) δ: 1.05(1H, m), 1.18–1.30(2H, m), 1.38–1.47(2H, m),1.54–1.81 (4H, m), 1.98–2.20(5H, m), 2.31(3H, s), 2.34(2H, t, J=7.5 Hz),2.51(1H, m), 3.70(3H, s), 3.80(1H, m), 4.16(2H, s), 5.29–5.42(2H, m),5.95 (1H, d, J=7.2 Hz), 6.78(1H, d, J=3.6 Hz), 6.96–7.11(3H, m),7.37(1H, d, J=3.6 Hz). IR(CHCl₃): 3514, 3446, 3427, 2669, 1709, 1641,1543, 1506, 1473, 1458, 1259, 1011 cm⁻¹. [α]_(D) ²⁴+62.7±1.0°(c=1.009,MeOH) Anal. (C₂₈H₃₅NO₄S) Calcd.(%): C, 69.82; H, 7.32; N, 2.91; S, 6.66.Found(%): C, 69.55; H, 7.27; N, 3.09; S, 6.55.

Compound Number I-227

¹H-NMR(CDCl₃) δ: 1.07(1H, m), 1.24–1.28(2H, m), 1.41–1.46(2H, m),1.56–1.79(4H, m), 2.00–2.17(5H, m), 2.16(3H, s), 2.33(2H, t, J=7.5 Hz),2.51 (1H, m), 3.79(1H, m), 4.08(2H, s), 5.28–5.42(2H, m), 6.05(1H, d,J=7.5 Hz), 6.75 (1H, d, J=3.6 Hz), 7.16(2H, d, J=8.1 Hz), 7.37(1H, d,J=3.6 Hz), 7.43 (2H, d, J=8.1 Hz), 7.53(1H, br s). IR(CHCl₃): 3512,3437, 1707, 1639, 1543, 1516, 1410 cm⁻¹. [α]_(D)^(24.5)+60.7±1.0°(c=1.012, MeOH) Anal. (C₂₈H₃₄N₂O₄S.0.5H₂O) Calcd.(%):C, 67.77; H, 7.00; N, 5.56; S, 6.37. Found(%): C, 66.84; H, 6.91; N,5.56; S, 6.26.

Compound Number I-228

¹H-NMR(CDCl₃) δ: 1.06(1H, m), 1.22–1.29(2H, m), 1.41–1.46(2H, m),1.58–1.76 (4H, m), 2.01–2.17(5H, m), 2.34(2H, t, J=7.5 Hz), 2.51(1H, m),2.99 (3H, s), 3.80(1H, m), 4.11(2H, s), 5.29–5.43(2H, m), 6.01(1H, d,J=7.5 Hz), 6.78(1H, d, J=3.6 Hz), 6.86(1H, br s), 7.17–7.23(4H, m),7.36(1H, d, J=3.6 Hz). IR(CHCl₃): 3510, 3444, 3427, 3371, 1709, 1639,1543, 1510, 1456, 1389, 1338, 1155 cm⁻¹. [α]_(D)^(24.5)+56.5±1.0°(c=0.953, MeOH) Anal. (C₂₇H₃₄N₂O₅S₂.0.1H₂O) Calcd.(%):C, 60.90; H, 6.47; N, 5.26; S, 12.04. Found(%): C, 61.06; H, 6.45; N,5.29; S, 11.52.

Compound Number I-229

mp.103–105° C.; ¹H-NMR(CDCl₃) δ: 1.02 (1H, m), 1.15–1.27 (2H, m),1.37–1.45(2H, m), 1.53–1.77(4H, m), 1.96–2.18(5H, m), 2.33 (2H, t, J=7.5Hz), 2.49(1H, m), 3.79(1H, m), 4.40(2H, s), 5.27–5.39 (2H, m), 5.94(1H,d, J=7.8 Hz), 6.89(1H, d, J=3.9 Hz), 7.32–7.37(2H, m), 7.43–7.48 (3H,m), 7.84(1H, m), 8.08(1H, d, J=6.9 Hz), 8.15(1H, m). IR(CHCl₃): 3514,3444, 3427, 2667, 1739, 1709, 1643, 1543, 1506, 1458, 1444 cm⁻¹. [α]_(D)^(24.5)+58.9±1.0°(c=1.006, MeOH) Anal. (C₃₂H₃₃NO₃S₂) Calcd.(%): C,70.68; H, 6.12; N, 2.58; S, 11.79. Found(%): C, 70.52; H, 6.11; N, 2.67;S, 11.72.

Compound Number I-230

mp.86–87° C.; ¹H-NMR(CDCl₃) δ: 1.02(1H, m), 1.16–1.28(2H, m), 1.37–1.45(2H, m), 1.54–1.77(4H, m), 1.97–2.17(5H, m), 2.32(2H, t, J=7.5 Hz), 2.49(1H, m), 3.78(1H, m), 3.79 and 4.26(each 2H, each s), 5.27–5.39(2H, m),5.93 (1H, d, J=7.2 Hz), 6.78(1H, d, J=3.9 Hz), 7.18(1H, d, J=7.2 Hz),7.29 (1H, m), 7.34–7.40(3H, m), 7.52(1H, d, J=7.2 Hz), 7.72(1H, d, J=7.5Hz), 7.78(1H, d, J=7.2 Hz). IR(CHCl₃): 3514, 3446, 3427, 2669, 1709,1641, 1543, 1506, 1456 cm⁻¹. [α]_(D) ^(24.5)+59.2±1.0°(c=1.006, MeOH)Anal. (C₃₃H₃₅NO₃S) Calcd.(%): C, 75.40; H, 6.71; N, 2.66; S, 6.10.Found(%): C, 75.33; H, 6.73; N, 2.75; S, 6.06.

Compound Number I-231

¹H-NMR (CHCl₃) δ: 1.04(1H, m), 1.16–1.30(2H, m), 1.38–1.46(2H, m),1.54–1.81(4H, m), 1.98–2.16(5H, m), 2.21 and 2.50(each 3H, each s), 2.34(2H, t, J=7.2 Hz), 2.51(1H, m), 3.66(3H, s), 3.80(1H, m), 4.13(2H, s),5.29–5.42 (2H, m), 5.93(1H, d, J=6.9 Hz), 6.78(1H, d, J=3.6 Hz), 6.89and 6.96 (each 1H, each d, each J=7.5 Hz), 7.36(1H, d, J=3.6 Hz).IR(CHCl₃): 3516, 3446, 3425, 2669, 1709, 1641, 1545, 1506, 1458, 1263,1084, 1009 cm⁻¹. [α]D²⁴+61.8±1.0°(c=1.006, MeOH) Anal.(C₂₉H₃₇NO₄S.0.2H₂O) Calcd.(%): C, 69.76; H, 7.55; N, 2.81; S, 6.42.Found(%): C, 69.80; H, 7.59; N, 2.97; S, 6.34.

Compound Number I-232

¹H-NMR(CDCl₃) δ: 1.02(1H, m), 1.16–1.27(2H, m), 1.37–1.45(2H, m),1.53–1.77(4H, m), 1.96–2.15(5H, m), 2.33(2H, t, J=7.5 Hz), 2.50(1H, m),3.79 (1H, m), 4.50(2H, s), 5.27–5.40(2H, m), 5.94(1H, d, J=7.5 Hz),6.88(1H, d, J=3.9 Hz), 7.29–7.38(4H, m), 7.47(1H, m), 7.58(1H, d, J=8.4Hz), 7.86(1H, m), 7.95(1H, d, J=7.8 Hz). IR(CHCl₃): 3512, 3444, 3427,2669, 1739, 1708, 1641, 1543, 1506, 1475, 1452, 1423 cm⁻¹. [α]_(D)²⁴+58.5±1.0°(c=1.006, MeOH) Anal. (C₃₂H₃₃NO₄S.0.2H₂O) Calcd.(%): C,72.34; H, 6.34; N, 2.64; S, 6.04. Found(%): C, 72.36; H, 6.16; N, 2.72;S, 5.94.

Compound Number I-233

mp.125–126° C.; ¹H-NMR(CDCl₃) δ: 1.05(1H, m), 1.18–1.28(2H, m),1.41–1.45 (2H, m), 1.57–1.78(4H, m), 2.00–2.20 (5H, m), 2.33(2H, t,J=7.4 Hz), 2.51 (1H, s), 3.80(1H, m),4.05 (2H, s), 5.28–5.42 (2H, m),5.98(1H, d, J=6.6 Hz), 6.76 (1H, d, J=3.6 Hz), 6.80 and 7.09(each 2H,each d, J=8.4 Hz), 7.37(1H, d, J=3.6 Hz). IR(KBr): 3354, 3132, 2688,1703, 1616, 1599, 1549, 1514, 1458, 1250 cm⁻¹. [α]_(D)²⁵+67.7±1.1°(c=1.001, MeOH) Anal. (C₂₆H₃₁NO₄S) Calcd.(%): C, 68.85; H,6.89; N, 3.09; S, 7.07. Found(%): C, 69.12; H, 6.95; N, 3.10; S, 7.12.

Compound Number II-1

¹H-NMR(CDCl₃) δ: 0.93(1H, d, J=10.2 Hz), 1.08 and 1.21(each 3H, each s),1.50–2.41(14H, m), 4.20(1H, m), 5.35–5.47(2H, m), 6.16(1H, d, J=8.7 Hz),6.33 and 7.16(each 2H, each t, each J=2.4 Hz), 7.30 and 7.56 (each 1H,each d, each J=3.9 Hz). IR(CHCl₃): 3515, 3446, 3144, 3100, 1708, 1658,1529, 1504, 1456, 1385, 1167 cm⁻¹. [α]_(D) ^(26.5)+54.1±0.9°(c=1.004,MeOH) Anal. (C₂₅H₃₂N₂O₅S₂.0.2H₂O) Calcd.(%): C, 59.08; H, 6.43; N, 5.51;S, 12.62. Found(%): C, 59.12; H, 6.36; N, 5.57; S, 12.59.

Compound Number II-6

¹H-NMR(CDCl₃) δ: 0.98(1H, d, J=10.2 Hz), 1.14 and 1.24(each 3H, each s),1.54–2.48(14H, m), 4.30(1H, m), 5.35–5.52(2H, m), 6.26 (1H, d, J=8.7Hz), 6.38 and 7.13 (each 2H, each t, J=2.1 Hz), 7.44 and 7.79 (each 2H,each d, each J=8.4 Hz). IR(CHCl₃): 3453, 2662, 1739, 1708, 1652, 1609,1500, 1333 cm⁻¹. [α]_(D) ²²+65.2±1.1°(c=1.006, MeOH) Anal.(C₂₇H₃₄N₂O₃.0.3H₂O) Calcd.(%): C, 73.71; H, 7.93; N, 6.37. Found(%): C,73.85; H, 7.88; N, 6.37.

Compound Number II-7

¹H-NMR(CDCl₃) δ: 0.95(1H, d, J=10.2 Hz), 1.10 and 1.22 (each 3H, eachs), 1.52–2.42(14H, m), 4.25(1H, m), 5.34–5.51(2H, m), 6.35(1H, d, J=8.7Hz), 7.07–7.15(3H, m), 7.21–7.26(2H, m), 7.73 and 7.77(each 2H, each d,each J=8.7 Hz). IR(CHCl₃): 3518, 3446, 3365, 3249, 2673, 1709, 1655,1516, 1348, 1167 cm⁻¹. [α]_(D) ^(21.5)+56.1±0.9°(c=1.000, MeOH) Anal.(C₂₉H₃₆N₂O₅S.0.6H₂O) Calcd.(%): C, 65.05; H, 7.00; N, 5.23; S, 5.99.Found(%): C, 65.07; H, 6.94; N, 5.37; S, 6.03.

Compound Number II-8

¹H-NMR(CDCl₃) δ: 0.89(1H, d, J=10.2 Hz), 1.05 and 1.19(each 3H, each s),1.50–2.44(14H, m), 4.15(1H, m), 5.31–5.50(2H, m), 6.31 (1H, d, J=8.1Hz), 7.00(1H, d, J=1.8 Hz), 7.42–7.47(2H, m), 7.54 (1H, d, J=1.8 Hz),7.56(1H, m), 7.76–7.79(2H, m), 8.29(1H, s). IR (CHCl₃): 3509, 3446,3360, 3108, 1708, 1639, 1515, 1448, 1330, 1164 cm⁻¹. [α]_(D)²⁰+39.0±0.8°(c=1.006, MeOH) Anal. (C₂₇H₃₄N₂O₅S₂.0.2H₂O) Calcd.(%): C,60.09; H, 6.54; N, 5.19; S, 11.88. Found(%): C, 60.07; H, 6.48; N, 5.31;S, 11.92.

Compound Number II-9

¹H-NMR(CDCl₃) δ: 0.73(1H, d, J=10.2 Hz), 1.06 and 1.16(each 3H, each s),1.43–2.36(14H, m), 4.07(1H, m), 5.28–5.49(2H, m), 6.37 (1H, d, J=8.7Hz), 7.28 and 7.33(each 1H, each d, each J=1.8 Hz), 7.38–7.43 (2H, m),7.50(1H, m), 7.96–7.99(2H, m). IR(CHCl₃): 3440, 3254, 3096, 3062, 1708,1643, 1560, 1530, 1298 cm⁻¹. [α]_(D) ²⁰+49.0±0.9°(c=1.008, MeOH) Anal.(C₂₈H₃₄N₂O₄S.0.4H₂O) Calcd.(%): C, 67.01; H, 6.99; N, 5.58; S, 6.39.Found(%): C, 66.96; H, 7.04; N, 5.67; S, 6.32.

Compound Number II-10

¹H-NMR(CDCl₃) δ: 0.96(1H, d, J=10.5 Hz), 1.09 and 1.22(each 3H, each s),1.52–2.44(14H, m), 4.26(1H, m), 5.33–5.49(2H, m), 6.26(1H, d, J=8.4 Hz),6.31 and 7.15(each 2H, each t, each J=2.1 Hz), 7.81 and 7.89 (each 2H,each d, each J=8.4 Hz). IR(CHCl₃): 3514, 3446, 3144, 1708, 1663, 1514,1377, 1173 cm⁻¹. [α]_(D) ²²+64.1±0.9°(c=1.000, MeOH) Anal.(C₂₇H₃₄N₂O₅S.0.2H₂O) Calcd.(%): C, 64.57; H, 6.90; N, 5.58; S, 6.38.Found(%): C, 64.50; H, 6.97; N, 5.71; S, 6.28.

Compound Number II-11

¹H-NMR(CDCl₃) δ: 0.94(1H, d, J=10.2 Hz), 1.08 and 1.21(each 3H, each s),1.50–2.43(14H, m), 4.12(2H, s), 4.22(1H, m), 5.33–5.49(2H, m), 6.06(1H,d, J=8.7 Hz), 7.04(1H, d, J=1.2 Hz), 7.22–7.34(2H, m), 7.63 (1H, d,J=1.2 Hz). IR(CHCl₃): 3517, 3451, 3087, 3065, 2670, 1708, 1708, 1647,1549, 1508 cm⁻¹. [α]_(D) ^(21.5)+41.9±0.8°(c=1.015, MeOH) Anal.(C₂₈H₃₅NO₃S) Calcd.(%): C, 72.22; H, 7.58; N, 3.01; S, 6.89. Found(%):C, 72.07; H, 7.57; N, 3.21; S, 6.77.

Compound Number II-12

¹H-NMR(CDCl₃) δ: 0.94(1H, d, J=10.5 Hz), 1.09 and 1.21(each 3H, each s),1.50–2.44 (14H, m), 4.24(1H, m), 5.32–5.48(2H, m), 6.24(1H, d, J=8.7Hz), 7.17 and 7.60(each 2H, each d, each J=8.7 Hz), 7.41–7.46 (2H, m),7.54(1H, m), 7.80–7.84(2H, m). IR(CHCl₃): 3510, 3451, 3371, 3139, 1709,1647, 1609, 1496, 1163 cm⁻¹. [α]_(D) ^(22.5)+47.1±0.9°(c=1.006, MeOH)Anal. (C₂₉H₃₆N₂O₅S.0.4H₂O) Calcd.(%): C, 65.49; H, 6.97; N, 5.27; S,6.03. Found(%): C, 65.51; H, 6.87; N, 5.39; S, 5.89.

Compound Number II-14

¹H-NMR(CHCl₃) δ: 0.92(1H, d, J=10.2 Hz), 1.09 and 1.21(each 3H, each s),1.53–2.47(14H, m), 4.17(1H, m), 5.35–5.55(2H, m), 6.35 and 7.17 (each2H, each t, each J=2.1 Hz), 6.38(1H, d, J=8.7 Hz), 8.09 and 8.17 (each1H, each d, each J=1.5 Hz). IR(CHCl₃): 3510, 3409, 3144, 3107, 1727,1.709, 1657, 1538, 1503, 1456, 1387, 1166 cm⁻¹. [α]_(D)²⁵+46.1±0.9°(c=1.005, MeOH) Anal. (C₂₅H₃₂N₂O₅S₂.0.2H₂O) Calcd.(%): C,59.08; H, 6.43; N, 5.51; S, 12.62. Found(%): C, 59.10; H, 6.45; N, 5.69;S, 12.58.

Compound Number II-15

mp.119–121° C. ¹H-NMR(CDCl₃) δ: 0.97(1H, d, J=10.2 Hz), 1.11 and1.24(each 3H, each s), 1.53–2.49(14H, m), 4.29(1H, m), 5.39–5.57 (2H,m), 6.37 and 7.22(each 2H, each t, each J=2.1 Hz), 7.13 (1H, d, J=8.4Hz), 7.50 and 7.93(each 1H, each d, each J=3.9 Hz). IR(Nujol): 3365,3145, 3100, 1739, 1621, 1548, 1405, 1367, 1187 cm⁻¹. [α]_(D)^(26.5)+45.5±0.8°(c=1.012, MeOH) Anal. (C₂₅H₃₂N₂O₅S₂) Calcd.(%): C,59.74; H, 6.02; N, 5.57; S, 12.76. Found(%): C, 59.56; H, 6.33; N, 5.64;S, 12.76.

Compound Number II-17

¹H-NMR(CDCl₃) δ: 0.96 (1H, d, J=10.5 Hz), 1.11 and 1.23(each 3H, eachs), 1.54–2.49(14H, m), 4.25(1H, m), 5.35–5.56(2H, m), 6.33 (2H, t, J=2.4Hz), 6.56(1H, d, J=7.8 Hz), 7.17(2H, t, J=2.4 Hz), 7.58(1H, t, J=7.8Hz), 7.93(1H, m), 8.04(1H, d, J=7.8 Hz), 8.24(1H, m). IR (CHCl₃): 3513,3389, 3144, 2669, 1726, 1709, 1659, 1515, 1470, 1455, 1375 cm⁻¹. [α]_(D)²⁵+54.0±0.9°(c=1.008, MeOH) Anal. (C₂₇H₃₄N₂O₅S.0.2H₂O) Calcd.(%): C,64.46; H, 6.90; N, 5.53; S, 6.38. Found(%): C, 64.45; H, 6.89; N, 5.75;S, 6.42.

Compound Number II-18

¹H-NMR(CDCl₃) δ: 0.96(1H, d, J=10.2 Hz), 1.10 and 1.23(each 3H, each s),1.52–2.42(14H, m), 2.29(3H, t), 4.26(1H, m), 5.35–5.49(2H, m), 5.96(1H,brs), 6.19(1H, t, J=3.2 Hz), 6.26(1H, d, J=8.1 Hz), 7.25 (1H, m),7.81(4H, s). IR(CHCl₃): 3511, 3446, 3152, 1708, 1662, 1514, 1485, 1368,1164 cm⁻¹. [α]_(D) ²⁷+59.4±1.0°(c=1.006, MeOH) Anal. (C₂₈H₃₆N₂O₅S)Calcd.(%): C, 65.60; H, 7.08; N, 5.46; S, 6.25. Found(%): C, 65.41; H,7.00; N, 5.67; S, 6.24.

Compound Number II-19

¹H-NMR(CDCl₃) δ: 0.97(1H, d, J=10.5 Hz), 1.03 and 1.22(each 3H, each s),1.452–2.46 (14H, m), 4.26(1H, m), 5.33–5.50(2H, m), 6.20 (2H, t, J=2.1Hz), 6.22(1H, d, J=8.1 Hz), 6.68(2H, t, J=2.1 Hz), 7.15 and 7.67 (each2H, each d, each J=8.1 Hz). IR(CHCl₃): 3511, 3452, 3103, 2666, 1709,1652, 1523, 1496 cm⁻¹. [α]_(D) ²³+57.7±1.0°(c=1.010, MeOH) Anal.(C₂₈H₃₆N₂O₃.0.1H₂O) Calcd.(%): C, 74.67; H, 8.10; N, 6.22. Found(%): C,74.69; H, 8.21; N, 6.38.

Compound Number II-20

¹H-NMR(CDCl₃) δ: 0.94(1H, d, J=10.2 Hz), 1.06 and 1.20(each 3H, each s),1.49–2.40(14H, m), 4.21(1H, m), 5.31–5.45(2H, m), 6.19(1H, d, J=8.4 Hz),6.88(1H, d, J=3.6 Hz), 7.22–7.35(2H, m), 7.52–7.55(2H, m), 7.74 and7.91(each 2H, each d, each J=8.4 Hz), 7.98(1H, d, J=8.4 Hz). IR(CHCl₃):3481, 3440, 3145, 3116, 2661, 1709, 1660, 1516, 1485, 1446, 1377, 1261,1178, 1130 cm⁻¹. [α]_(D) ²⁶+56.6±1.0°(c=1.000, MeOH) Anal.(C₃₁H₃₆N₂O₅S.0.1H₂O) Calcd.(%): C, 67.64; H, 6.63; N, 5.09; S, 5.82.Found(%): C, 67.68; H, 6.72; N, 5.35; S, 5.73.

Compound Number II-21

¹H-NMR(CDCl₃) δ: 0.95(1H, d, J=10.2 Hz), 1.09 and 1.22 (each 3H, eachs), 1.52–2.45(14H, m), 4.24(1H, m), 4.63(2H, s), 5.34–5.50(2H, m),6.25–6.27(2H, m), 6.40(1H, d, J=8.4 Hz), 7.25(1H, dd, J=1.8 and 3.0 Hz),7.80 and 7.85(each 2H, each d, each J=8.7 Hz). IR(CHCl₃): 3581, 3518,3445, 3149, 2666, 1709, 1661, 1515, 1472, 1371, 1182, 1150 cm⁻¹. [α]_(D)²⁷+58.1±1.0°(c=1.007, MeOH) Anal. (C₂₈H₃₆N₂O₆S) Calcd.(%): C, 63.61; H,6.86; N, 5.30; S, 6.07. Found(%): C, 63.50; H, 6.84; N, 5.44; S, 5.89.

Compound Number II-31

mp.98–100° C. ¹H-NMR(CDCl₃) δ: 0.94(1H, d, J=10.2 Hz), 1.08 and1.21(each 3H, each s), 1.50–2.43(14H, m), 4.13(2H, s), 4.20 (1H, m),5.33–5.49(2H, m), 5.97(1H, d, J=8.4 Hz), 6.77(1H, m), 7.21–7.35(6H, m).IR(KBr): 3407, 2674, 1703, 1630, 1511 cm⁻¹. [α]_(D)²⁴+46.8±0.9°(c=1.006, MeOH) Anal. (C₂₈H₃₅NO₃S) Calcd.(%): C, 72.22; H,7.58; N, 3.01; S, 6.89. Found(%): C, 72.04; H, 7.36; N, 3.27; S, 6.91.

Compound Number II-37

¹H-NMR(CDCl₃) δ: 0.93(1H, d, J=10.5 Hz), 1.08 and 1.21(each 3H, each s),1.50–2.41(14H, m), 4.20(1H, m), 5.39–5.47(2H, m), 6.19(1H, d, J=8.4 Hz),7.35(1H, d, J=3.9 Hz), 7.51–7.64(4H, m), 7.98(2H, m). IR(CHCl₃): 3516,3446, 2667, 1709, 1657, 1529, 1504, 1327, 1157 cm⁻¹. [α]_(D)²⁰+55.6°±1.0°(c=1.004, MeOH) Anal. (C₂₇H₃NO₅S.0.2H₂O) Calcd.(%) C,62.45; H, 6.48; N, 2.70; S, 12.35. Found(%): C, 62.46; H, 6.40; N, 2.75;S, 12.19.

Compound Number II-47

¹H-NMR(CDCl₃) δ: 0.93(1H, d, J=10.2 Hz), 1.08 and 1.21(each 3H, each s),1.50–2.41(14H, m), 4.21(1H, m), 5.34–5.48(2H, m), 6.21(1H, d, J=8.4 Hz),7.36 and 7.63(each 1H, each d, each J=3.9 Hz), 7.70(1H, dd, J=1.5 and5.1 Hz), 7.75(1H, dd, J=1.5 and 3.9 Hz). IR(CHCl₃): 3516, 3446, 3097,1708, 1656, 1529, 1504, 1337, 1153 cm⁻¹. [α]_(D) ²⁵+54.1±0.9°(c=1.000,MeOH) Anal. (C₂₅H₃₁NO₅S₃) Calcd.(%): C, 57.56; H, 5.99; N, 2.68; S,18.44. Found(%): C, 57.33; H, 5.95; N, 2.68; S, 18.38.

Compound Number II-55

¹H-NMR(CDCl₃) δ: 0.93(1H, d, J=10.5 Hz), 1.08 and 1.22(each 3H, each s),1.50–2.41(14H, m), 2.39(3H, d, J=0.6 Hz), 4.21(1H, m), 5.35–5.48(2H, m),5.99(1H, m), 6.15(1H, d, J=8.7 Hz), 6.20(1H, t, J=3.3 Hz), 7.18(1H, dd,J=1.8 and 3.3 Hz), 7.31 and 7.54(each 1H, each d, each J=3.9 Hz).IR(CHCl₃): 3511, 3446, 3150, 3101, 1708, 1658, 1529, 1504, 1375, 1183,1160 cm⁻¹. [α]_(D) ²³+50.3±0.9°(c=1.007, MeOH) Anal.(C₂₆H₃₄N₂O₅S₂.0.2H₂O) Calcd.(%): C, 59.79; H, 6.64; N, 5.36; S, 12.28.Found(%): C, 59.72; H, 6.61; N, 5.51; S, 12.37.

Compound Number II-59

¹H-NMR(CDCl₃) δ: 0.93(1H, d, J=10.2 Hz), 1.07 and 1.21(each 3H, each s),1.49–2.41(14H, m), 4.19(1H, m), 5.33–5.47(2H, m), 5.99(1H, d, J=8.7 Hz),7.01(1H, dd, J=3.6 and 5.4 Hz), 7.04 and 7.28(each 1H, each d, eachJ=3.6 Hz), 7.29(1H, dd, J=1.2 and 3.6 Hz), 7.43(1H, dd, J=1.2 and 5.4Hz). IR(CHCl₃): 3518, 3449, 3430, 2672, 1708, 1646, 1530, 1500, 1421cm⁻¹. [α]_(D) ^(25.5)+45.9±0.9°(c=1.010, MeOH) Anal. (C₂₅H₃₁NO₃S₃)Calcd.(%): C, 61.32; H, 6.38; N, 2.86; S, 19.64. Found(%): C, 61.17; H,6.42; N, 3.00; S, 19.80.

Compound Number II-60

¹H-NMR (CHCl₃) δ: 0.96 (1H,d,J=10.2 Hz),1.10 and 1.22 (each 3H, each s),1.51–1.79 (3H, m), 1.83–2.44 (11H, m), 4.26 (1H, m), 5.33–5.49 (2H, m),6.21 (1H, d, J=8.7 Hz), 7.25 (2H, d, J=9.0 Hz), 7.34–7.47 (5H,m), 7.60(2H, d, J=9.0 Hz) IR (CHCl₃): 3453, 3062, 3029, 3014, 2925, 2870, 1739,1708, 1651, 1595, 1583, 1557, 1515, 1481 cm⁻¹. [α]_(D)²²+61.0°(c=1.01,CH₃OH) Anal. (C₂₉H₃₅NO₃S.0.1H₂O) Calcd.(%): C, 72.65; H,7.48; N, 2.92; S, 6.69. Found (%): C, 72.50; H, 7.45; N, 3.19; S, 6.69.

Compound Number II-81

¹H-NMR(CDCl₃) δ: 0.93(1H, d, J=10.2 Hz), 1.07 and 1.21(each 3H, each s),1.49–2.41(14H, m), 2.46(3H, d, J=1.2 Hz), 4.18(1H, m), 5.33–5.47(2H, m),5.99(1H, d, J=8.4 Hz), 6.66(1H, m), 6.99(1H, d, J=3.9 Hz), 7.10(1H, d,J=3.3 Hz), 7.26(1H, d, J=3.9 Hz). IR(CHCl₃): 3509, 3449, 2671, 1708,1645, 1530, 1500, 1420 cm⁻¹. [α]_(D) ^(25.5)+43.5±0.8°(c=1.002, MeOH)Anal. (C₂₆H₃₃NO₃S₃) Calcd.(%): C, 61.99; H, 6.60; N, 2.78; S, 19.10.Found(%): C, 61.77; H, 6.68; N, 2.83; S, 18.91.

Compound Number II-82

mp.118–120° C. ¹H-NMR(CDCl₃) δ: 0.94(1H, d, J=10.2 Hz), 1.09 and1.22(each 3H, each s), 1.51–2.42(14H, m), 2.53(3H, d, J=0.9 Hz), 4.20(1H, m), 5.35–5.48(2H, m), 6.17(1H, d, J=8.7 Hz), 6.77(1H, m), 7.34 (1H,d, J=3.9 Hz), 7.57(1H, d, J=3.6 Hz), 7.60(1H, d, J=3.9 Hz). IR (Nujol):3399, 3082, 1733, 1613, 1543, 1328, 1318, 1151 cm⁻¹. [α]_(D)^(25.5)+54.0±0.9°(c=1.012, MeOH) Anal. (C₂₆H₃₃NO₅S₃) Calcd.(%): C,58.29; H, 6.21; N, 2.61; S, 17.95. Found(%): C, 58.08; H, 6.18; N, 2.73;S, 17.66.

Compound Number II-88

mp.91–92° C. ¹H-NMR(CDCl₃) δ: 0.95(1H, d, J=10.5 Hz), 1.09 and 1.22(each3H, each s),1.51–2.44(14H, m), 4.16(2H, s), 4.20 (1H, m), 5.34–5.49(2H,m), 5.99(1H, d, J=8.7 Hz), 6.79(1H, d, J=3.9 Hz), 6.96 (1H, dd, J=1.2and 4.8 Hz), 7.05(1H, m), 7.28(1H, dd, J=3.0 and 4.8 Hz), 7.32(1H, d,J=3.9 Hz). IR(Nujol): 3408, 2677, 1703, 1626, 1541, 1514, 1246 cm⁻¹.[α]_(D) ²⁶+43.8±0.8°(c=1.005, MeOH) Anal. (C₂₆H₃₃NO₃S₂) Calcd.(%): C,66.21; H, 7.05; N, 2.97; S, 13.60. Found(%): C, 66.00; H, 7.81; N, 3.11;S, 13.69.

Compound Number II-92

mp.165–166° C. ¹H-NMR(CDCl₃) δ: 0.93(1H, d, J=10.2 Hz), 1.08 and1.20(each 3H, each s), 1.50–2.45(14H, m), 4.17(1H, m), 5.33–5.51(2H, m),6.04(1H, d, J=8.4 Hz), 6.51(1H, dd, J=1.5 and 3.3 Hz), 7.15(1H, dd,J=2.4 and 3.3 Hz), 7.52–7.57(2H, m), 7.65(1H, m), 7.74(1H, dd, J=1.8 and2.1 Hz), 7.89–7.93(1H, m). IR(CHCl₃): 3510, 3449, 3144, 1733, 1708,1650, 1570, 1507, 1384, 1185, 1176 cm⁻¹. [α]_(D) ²⁴+33.8±0.7°(c=1.011,MeOH) Anal. (C₂₇H₃₄N₂O₅S) Calcd.(%): C, 65.04; H, 6.87; N, 5.62; S,6.43. Found(%): C, 64.95; H, 6.68; N, 5.69; S, 6.40.

Compound Number II-93

¹H-NMR(CDCl₃) δ: 0.93(1H, d, J=10.2 Hz), 1.08 and 1.21(each 3H, each s),150–2.46(14H, m), 4.19(1H, m), 5.33–5.50(2H, m), 6.03(1H, d, J=8.7 Hz),6.52(1H, dd, J=1.5 and 3.3 Hz), 7.11(1H, dd, J=3.9 and 4.8 Hz), 7.17(1H,dd, J=2.1 and 3.3 Hz), 7.70–7.72(2H, m), 7.74(1H, dd, J=1.2 and 3.9 Hz).IR(CHCl₃): 3510, 3448, 3143, 2666, 1733, 1708, 1650, 1572, 1507, 1387,1179 cm⁻¹. [α]_(D) ²⁴+39.1°±0.8° (c=1.003, MeOH) Anal. (C₂₅H₃₂N₂O₅S₂)Calcd.(%): C, 59.50; H, 6.39; N, 5.55; S, 12.71. Found(%): C, 59.49; H,6.46; N, 5.47; S, 12.70.

Compound Number II-94

mp.132–133° C. 300 MHz ¹H-NMR(CDCl₃) δ: 0.93(1H, d, J=10.2 Hz), 1.08 and1.21(each 3H, each s), 1.54–2.44(14H, m), 4.19(1H, m), 5.33–5.50 (2H,m), 6.03(1H, d, J=8.7 Hz), 6.52(1H, dd, J=1.5 and 3.3 Hz), 7.11(1H, dd,J=3.9 and 4.8 Hz), 7.17(1H, dd, J=2.1 and 3.3 Hz), 7.70–7.72(2H, m),7.74(1H, dd, J=1.5 and 3.9 Hz). IR(CHCl₃): 3510, 3448, 3143, 3099, 1733,1708, 1650, 1572, 1507, 1473, 1387, 1179 cm⁻¹. [α]_(D)²⁴+39.1±0.8°(c=1.003, MeOH) Anal. (C₂₅H₃₂N₂O₅S₂) Calcd.(%): C, 59.50; H,6.39; N, 5.55; S, 12.71. Found(%): C, 59.49; H, 6.46; N, 5.47; S, 12.70.

Compound Number II-98

mp.138–139° C. ¹H-NMR(CDCl₃) δ: 0.97(1H, d, J=10.2 Hz), 1.13 and1.24(each 3H, each s), 1.50–2.47(14H, m), 4.24(1H, m), 5.36–5.52 (2H,m), 6.06(1H, d, J=8.4 Hz), 6.98(1H, d, J=3.9 Hz), 6.99 and 7.05 (each1H, each d, each J=16.2 Hz), 7.28–7.34(3H, m), 7.37 (1H, d, J=3.9 Hz).IR(CHCl₃): 3518, 3449, 3431, 2665, 1708, 1642, 1538, 1519, 1500 cm⁻¹.[α]_(D) ²⁴+49.1±0.9°(c=1.014, MeOH) Anal. (C₂₇H₃₃NO₃S₂) Calcd.(%): C,67.05; H, 6.88; N, 2.90; S, 13.26. Found(%): C, 67.94; H, 6.86; N, 2.99;S, 13.23.

Compound Number II-99

¹H-NMR(CDCl₃) δ: 0.94(1H, d, J=9.9 Hz), 1.07 and 1.22 (each 3H, each s),1.50–2.44(14H, m), 4.20(1H, m), 5.30–5.51(2H, m), 5.97(1H, d, J=9.0 Hz),6.58(2H, s), 6.95(1H, d, J=3.9 Hz), 7.02(1H, dd, J=1.5 and 4.8 Hz),7.25–7.31(2H, m), 7.31(1H, d, J=3.9 Hz). IR(CHCl₃): 3517, 3449, 3430,2664, 1708, 1642, 1536, 1519, 1501 cm⁻¹. [α]_(D) ²⁴+38.6±0.8°(c=1.006,MeOH) Anal. (C₂₇H₃₃NO₃S₂.0.2H₂O) Calcd.(%): C, 66.55; H, 6.91; N, 2.87;S, 13.16. Found(%): C, 66.52; H, 6.81; N, 3.11; S, 12.93.

Compound Number II-100

¹H-NMR(CDCl₃) δ: 0.94(1H, d, J=10.2 Hz), 1.09 and 1.22(each 3H, each s),1.50–2.39(14H, m), 2.44(3H, d, J=0.9 Hz), 4.20(1H, m), 5.34–5.49(2H, m),5.98(1H, d, J=8.7 Hz), 6.70(1H, m), 7.06(1H, d, J=3.9 Hz), 7.10(1H, d,J=1.8 Hz), 7.30(1H, d, J=3.9 Hz). IR(CHCl₃): 3518, 3450, 3430, 3110,2669, 1740, 1708, 1645, 1530, 1499, 1420 cm⁻¹. [α]_(D)²⁴+46.0±0.9°(c=0.968, MeOH) Anal. (C₂₆H₃₃NO₃S₃) Calcd.(%): C, 61.99; H,6.60; N, 2.78; S, 19.10. Found(%): C, 61.99; H, 6.61; N, 2.87; S, 19.18.

Compound Number II-101

¹H-NMR(CDCl₃) δ: 0.94(1H, d, J=10.5 Hz), 1.09 and 1.22(each 3H, each s),1.51–2.42(14H, m), 2.47(3H, d, J=0.9 Hz), 4.21(1H, m), 5.35–5.49(2H, m),6.18(1H, d, J=8.7 Hz), 7.04(1H, m), 7.36 and 7.60(each 1H, each d, eachJ=3.9 Hz), 7.91(1H, d, J=1.5 Hz). IR(CHCl₃): 3510, 3447, 3115, 2670,1708, 1656, 1529, 1504, 1443, 1329, 1156, 1143 cm⁻¹. [α]_(D)²⁴+53.8±0.9°(c=1.008, MeOH) Anal. (C₂₆H₃₃NO₅S₃) Calcd.(%): C, 58.29; H,6.21; N, 2.61; S, 17.96. Found(%): C, 58.07; H, 6.05; N, 2.69; S, 17.94.

Compound Number II-102

¹H-NMR(CDCl₃) δ: 0.94(1H, d, J=10.2 Hz), 1.09 and 1.22(each 3H, each s),1.50–2.45(14H, m), 4.22(1H, m), 5.35–5.49(2H, m), 6.04(1H, d, J=8.7 Hz),6.52 and 6.69(each 1H, each d, each J=12.0 Hz), 6.99 (1H, dd, J=3.6 and5.1 Hz), 7.07(1H, d, J=3.9 Hz), 7.13(1H, d, J=3.9 Hz), 7.27(1H, dd,J=0.9 and 5.1 Hz) 7.36(1H, d, J=3.9 Hz). IR (CHCl₃): 3510, 3449, 3430,2664, 1708, 1643, 1536, 1501 cm⁻¹. [α]_(D) ²⁴+40.3±0.8°(c=1.011, MeOH)Anal. (C₂₇H₃₃NO₃S₂.0.3H₂O) Calcd.(%): C, 66.31; H, 6.92; N, 2.86; S,13.11. Found(%): C, 66.29; H, 6.81; N, 3.07; S, 13.13.

Compound Number II-103

mp.117–118° C. ¹H-NMR(CDCl₃) δ: 0.97(1H, d, J=10.2 Hz), 1.13 and1.24(each 3H, each s), 1.50–2.47(14H, m), 4.24(1H, m), 5.36–5.52(2H, m),6.06(1H, d, J=8.7 Hz), 6.97 and 7.15(each 1H, each d, each J=15.9 Hz),6.98(1H, d, J=3.9 Hz), 7.01(1H, dd, J=3.3 and 4.8 Hz), 7.09 (1H, d,J=3.3 Hz), 7.23(1H, d, J=4.8 Hz), 7.36(1H, d, J=3.9 Hz). IR(CHCl₃):3517, 3450, 2670, 1738, 1708, 1641, 1537, 1518, 1500 cm⁻¹. [α]_(D)²⁴+55.7±1.0°(c=1.001, MeOH) Anal. (C₂₇H₃₃NO₃S₂) Calcd.(%): C, 67.05; H,6.88; N, 2.90; S, 13.26. Found(%): C, 66.91; H, 6.83; N, 2.97; S, 13.13.

Compound Number II-107

¹H-NMR(CDCl₃) δ: 0.93(1H, d, J=10.2 Hz), 1.09 and 1.22(each 3H, each s),1.51–2.44(14H, m), 4.20(1H, m), 5.34–5.50(2H, m), 6.22 and 6.23(total1H, each d, J=8.1 and 8.7 Hz), 7.12(1H, dd, J=3.9 and 5.1 Hz), 7.44(2H,m), 7.60(1H, m), 7.69(1H, m). IR(CHCl₃): 3509, 3447, 3092, 1708, 1653,1530, 1503 cm⁻¹. [α]_(D) ²³+49.3±0.9°(c=1.002, MeOH) Anal.(C₂₅H₃₁NO₄S₃.0.4H₂O) Calcd.(%): C, 58.54; H, 6.25; N, 2.73; S, 18.75.Found(%): C, 58.62; H, 6.16; N, 2.88; S, 18.72.

Compound Number II-108

¹H-NMR(CDCl₃) δ: 0.94(1H, d, J=10.2 Hz), 1.09 and 1.10(total 3H, eachs), 1.22 and 1.23(total 3H, each s), 1.51–2.44(14H, m), 2.52 and2.53(total 3H, each d, J=0.6 Hz), 4.20(1H, m), 5.35–5.50(2H, m), 6.23and 6.24(total 1H, each d, J=8.7 and 8.4 Hz), 6.77(1H, m), 7.39–7.46(3H, m). IR (CHCl₃): 3510, 3447, 3429, 3093, 2665, 1708, 1652, 1530,1502, 1437 cm⁻¹. [α]_(D) ²³+47.4±0.9°(c=1.008, MeOH) Anal.(C₂₆H₃₃NO₄S₃.0.3H₂O) Calcd.(%): C, 59.47; H, 6.45; N, 2.67; S, 18.32.Found(%): C, 59.59; H, 6.16; N, 2.76; S, 18.11.

Compound Number II-112

¹H-NMR(CDCl₃) δ: 0.94(1H, d, J=10.2 Hz), 1.09 and 1.21(each 3H, each s),1.51–2.43(14H, m), 3.38(3H, s), 4.18(1H, m), 5.33–5.50(2H, m), 5.83(1H,d, J=8.7 Hz), 6.16(1H, d, J=3.9 Hz), 7.14(1H, m), 7.21–7.27 (4H, m),7.33–7.39(2H, m). IR(CHCl₃): 3514, 3450, 2661, 1739, 1709, 1628, 1597,1495, 1479, 1415, 1132 cm⁻¹. [α]_(D) ^(23.5)+50.8°±0.9° (c=1.005, MeOH)Anal. (C₂₈H₃₆N₂O₃S.0.2H₂O) Calcd.(%): C, 69.45; H, 7.58; N, 5.78; S,6.62. Found(%): C, 69.45; H, 7.39; N, 5.99; S, 6.65.

Compound Number II-113

¹H-NMR(CDCl₃) δ: 0.95(1H, d, J=10.5 Hz), 1.09 and 1.22(each 3H, each s),1.50–2.44(14H, m), 2.31(3H, s), 4.22(1H, m), 5.35–5.49(2H, m), 6.01(1H,d, J=8.7 Hz), 7.03–7.21(4H, m), 7.38(1H, d, J=3.9 Hz). IR(CHCl₃): 3516,3448, 3429, 1739, 1709, 1647, 1529, 1500, 1473, 1421 cm⁻¹. [α]_(D)²⁰+46.2°±1.0°(c=1.003, MeOH) Anal. (C₂₈H₃₅NO₃S₂.0.2H₂O) Calcd.(%): C,67.08; H, 7.12; N, 2.79; S, 12.79. Found(%): C, 67.12; H, 7.04; N, 2.94;S, 12.88.

Compound Number II-114

mp.112–115° C. ¹H-NMR(CDCl₃) δ: 0.93(1H, d, J=10.2 Hz), 1.08 and1.21(each 3H, each s), 1.50–2.39(14H, m), 2.42(3H, s), 4.20(1H, m),5.34–5.47(2H, m), 6.17(1H, d, J=8.7 Hz), 7.34(1H, d, J=3.9 Hz), 7.41(2H, m), 7.59(1H, d, J=3.9 Hz), 7.78(2H, m). IR(CHCl₃): 3516, 3446,1739, 1707, 1655, 1529, 1504, 1331, 1151 cm⁻¹. [α]_(D)²⁰+53.0°±0.9°(c=1.002, MeOH) Anal. (C₂₈H₃₅NO₅S₂.0.2H₂O) Calcd.(%): C,63.06; H, 6.69; N, 2.63; S, 12.02. Found(%): C, 63.07; H, 6.62; N, 2.73;S, 12.04.

Compound Number II-115

¹H-NMR(CDCl₃) δ: 0.95(1H, d, J=10.2 Hz), 1.09 and 1.22(each 3H, each s),1.50–2.44(14H, m), 3.77(3H, s), 4.22(1H, m), 5.35–5.49(2H, m), 6.04(1H,d, J=8.7 Hz), 6.74–6.89(3H, m), 7.17–7.23(2H, m), 7.40 (1H, d, J=3.9Hz). IR(CHCl₃): 3514, 3448, 3431, 1739, 1707, 1649, 1529, 1500, 1477cm⁻¹. [α]_(D) ²⁰+45.8°±0.9°(c=1.011, MeOH) Anal. (C₂₈H₃₅NO₄S₂.0.3H₂O)Calcd.(%): C, 64.78; H, 6.91; N, 2.70; S, 12.35. Found(%): C, 64.62; H,6.83; N, 2.85; S, 12.65.

Compound Number II-116

¹H-NMR(CDCl₃) δ: 0.93(1H, d, J=10.5 Hz), 1.08 and 1.21(each 3H, each s),1.50–2.41(14H, m), 3.86(3H, s), 4.20(1H, m), 5.34–5.47 (2H, m), 6.17(1H,d, J=8.7 Hz), 7.12(1H, m), 7.35(1H, d, J=3.9 Hz), 7.40–7.48(2H, m),7.56(1H, m), 7.60(1H, d, J=3.9 Hz). IR(CHCl₃): 3514, 3446, 2667, 1707,1657, 1599, 1529, 1504, 1481, 1329, 1252, 1151 cm⁻¹. [α]_(D)²⁰+52.6°±0.9°(c=1.011, MeOH) Anal. (C₂₈H₃₅NO₆S₂.0.2H₂O) Calcd.(%): C,61.22; H, 6.50; N, 2.55; S, 11.67. Found(%): C, 61.10; H, 6.36; N, 2.65;S, 11.73.

Compound Number II-117

¹H-NMR(CDCl₃) δ: 0.92(1H, d, J=10.5 Hz), 1.07 and 1.20(each 3H, each s),1.52–2.43(14H, m), 4.18(1H, m), 5.33–5.50(2H, m), 6.42(1H, d, J=8.4 Hz),7.07(1H, m), 7.33–7.39(2H, m), 7.46–7.51(2H, m), 7.56 (1H, d, J=3.9 Hz).IR(CHCl₃): 3587, 3442, 3280, 1707, 1643, 1531, 1329, 1308, 1149 cm⁻¹.[α]_(D) ²⁰+53.2°±0.9°(c=1.010, MeOH) Anal. (C₂₇H₃₃NO₆S₂.0.4H₂O)Calcd.(%): C, 60.18; H, 6.32; N, 2.60; S, 11.90. Found(%): C, 60.19; H,6.06; N, 2.63; S, 11.99.

Compound Number II-118

¹H-NMR(CDCl₃) δ: 0.91(1H, d, J=10.2 Hz), 1.08 and 1.21(each 3H, each s),1.50–2.45(14H, m), 4.20(1H, m), 5.33–5.50(2H, m), 6.17(1H, d, J=8.7 Hz),6.72(2H, m), 6.79(1H, m), 7.11(2H, m), 7.38(1H, d, J=3.9 Hz). IR(CHCl₃):3342, 2669, 1707, 1622, 1583, 1535 cm⁻¹. [α]_(D) ²³+45.6°±0.9°(c=1.007,MeOH) Anal. (C₂₇H₃₃NO₄S₂.0.2H₂O) Calcd.(%): C, 64.44; H, 6.69; N, 2.78;S, 12.74. Found(%): C, 64.33; H, 6.59; N, 2.83; S, 13.07.

Compound Number II-119

¹H-NMR(CDCl₃) δ: 0.94(1H, d, J=10.5 Hz), 1.08 and 1.21(each 3H, each s),1.50–2.43(14H, m), 3.79(3H, s), 4.10(2H, s), 4.20(1H, m), 5.33–5.49(2H,m), 5.98(1H, d, J=8.7 Hz), 6.76–6.85(4H, m), 7.24(1H, m), 7.32(1H, d,J=3.9 Hz). IR(CHCl₃): 3516, 3450, 3431, 2669, 1738, 1709, 1641, 1600,1437, 1261 cm⁻¹. [α]_(D) ^(23.5)+42.8°±0.8°(c=1.005, MeOH.) Anal.(C₂₉H₃₇NO₄S) Calcd.(%): C, 70.27; H, 7.52; N, 2.83; S, 6.47. Found(%):C, 70.05; H, 7.55; N, 2.84; S, 6.45.

Compound Number II-125

¹H-NMR(CDCl₃) δ: 0.93(1H, d, J=9.9 Hz), 1.08 and 1.21(each 3H, each s),1.50–2.42(14H, m), 2.28(3H, s), 4.12(2H, s), 4.20(1H, m), 5.33–5.48 (2H,m), 5.98(1H, d, J=9.0 Hz), 6.71(1H, d, J=3.6 Hz), 7.17 (4H, s), 7.30(1H,d, J=3.6 Hz). IR(CHCl₃): 3518, 3450, 3430, 1739, 1709, 1641, 1543, 1506,1471, 1458 cm⁻¹. [α]_(D) ^(22.5)+42.9°±0.8°(c=1.000, MeOH) Anal.(C₂₉H₃₇NO₃S) Calcd.(%): C, 72.61; H, 7.77; N, 2.92; S, 6.68. Found(%):C, 72.43; H, 7.78; N, 3.09; S, 6.62.

Compound Number II-126

¹H-NMR(CDCl₃) δ: 0.93(1H, d, J=10.5 Hz), 1.08 and 1.21(each 3H, each s),1.50–2.42(14H, m), 3.84(3H, s), 4.12(2H, s), 4.19(1H, m), 5.33–5.48 (2H,m), 5.98(1H, d, J=9.0 Hz), 6.77(1H, dt, J=0.9 and 3.9 Hz), 6.88(1H, d,J=8.1 Hz), 9.90(1H, m), 7.15(1H, m), 7.23(1H, m), 7.28(1H, d, J=3.9 Hz).IR(CHCl₃): 3509, 3450, 3431, 2664, 1739, 1708, 1639, 1544, 1506, 1464cm⁻¹. [α]_(D) ²⁴+40.4°±0.8°(c=1.003, MeOH) Anal. (C₂₉H₃₇NO₄S.0.1H₂O)Calcd.(%): C, 70.02; H, 7.53; N, 2.81; S, 6.45. Found(%): C, 69.92; H,7.53; N, 2.96; S, 6.46.

Compound Number II-127

¹H-NMR(CDCl₃) δ: 0.94(1H, d, J=10.5 Hz), 1.08 and 1.21(each 3H, eachs),1.18(3H, t, J=7.8 Hz), 1.50–2.42(14H, m), 2.64(2H, q, J=7.8 Hz),4.15(2H, s), 4.19(1H, m), 5.33–5.48(2H, m), 5.96(1H, d, J=9.3 Hz), 6.68(1H, d, J=3.6 Hz), 7.16–7.25(4H, m), 7.29(1H, d, J=3.6 Hz). IR (CHCl₃):3516, 3450, 3431, 2667, 1739, 1709, 1641, 1543, 1506, 1471, 1456 cm⁻¹.[α]_(D) ²¹+41.9±0.8°(c=1.013, MeOH) Anal. (C₃₀H₃₉NO₃S.0.1H₂O) Calcd.(%):C, 72.72; H, 7.97; N, 2.83; S, 6.47. Found(%): C, 72.55; H, 7.88; N,3.19; S, 6.62.

Compound Number II-129

¹H-NMR(CDCl₃) δ: 0.94(1H, d, J=9.9 Hz), 1.09 and 1.22(each 3H, eachs),1.50–2.42(14H, m), 2.43(3H, s), 4.20(1H, m), 4.24(2H, s), 5.34–5.49(2H, m), 5.99(1H, d, J=8.7 Hz), 6.58(1H, m), 6.67(1H, d, J=3.3 Hz),6.83(1H, d, J=3.9 Hz), 7.32(1H, d, J=3.9 Hz). IR (CHCl₃): 3516, 3450,3431, 2667, 1709, 1643, 1545, 1508, 1471, 1458 cm⁻¹. [α]_(D)²²+42.8±0.8°(c=1.006, MeOH) Anal. (C₂₇H₃₅NO₃S₂) Calcd.(%): C, 66.77; H,7.26; N, 2.88; S, 13.20. Found(%): C, 66.60; H, 7.23; N, 2.93; S, 13.19.

Compound Number II-132

¹H-NMR(CDCl₃) δ: 0.94(1H, d, J=10.5 Hz), 1.09 and 1.22(each 3H, each s),1.50–2.44(14H, m), 2.31(3H, s), 4.21(1H, m), 4.25(2H, s), 5.34–5.49 (2H,m), 6.01(1H, d, J=8.7 Hz), 6.83(1H, d, J=3.9 Hz), 7.03 (1H, m),7.11–7.20(3H, m), 7.27(1H, d, J=3.9 Hz). IR(CHCl₃): 3516, 3450, 3431,2665, 1739, 1709, 1643, 1543, 1508, 1473 cm¹. [α]_(D)²²+42.6±1.0°(c=0.861, MeOH) Anal. (C₂₉H₃₇NO₃S₂H₂O) Calcd.(%): C, 67.59;H, 7.31; N, 2.72; S, 12.44. Found(%): C, 67.49; H, 7.27; N, 2.82; S,12.35.

Compound Number II-133

¹H-NMR(CDCl₃) δ: 0.95(1H, d, J=10.5 Hz), 1.09 and 1.21(each 3H, each s),1.50–2.44(14H, m), 4.15(2H, s), 4.20(1H, m), 5.33–5.49(2H, m), 6.0(1H,d, J=9.3 Hz), 6.13(1H, dd, J=0.6 and 3.0 Hz), 6.32(1H, dd, J=1.8 and 3.0Hz), 6.84 and 7.22(each 1H, each d, each J=3.6 Hz), 7.47(1H, dd, J=0.6and 1.8 Hz). IR(CHCl₃): 3518, 3450, 3431, 2669, 1739, 1709, 1643, 1545,1506 cm⁻¹. [α]_(D) ²³+45.8±0.9°(c=1.003, MeOH) Anal. (C₂₆H₃₃NO₄S.0.6H₂O)Calcd.(%): C, 66.95; H, 7.39; N, 3.00; S, 6.87. Found(%): C, 67.04; H,7.17; N, 3.11; S, 7.03.

Compound Number II-134

¹H-NMR(CDCl₃) δ: 0.95(1H, d, J=10.5 Hz), 1.10 and 1.22(each 3H, each s),1.52–2.45(14H, m), 3.96(2H, s), 4.20(1H, m), 5.33–5.49(2H, m), 6.00(1H,d, J=8.7 Hz), 6.30(1H, dd, J=0.9 and 1.8 Hz), 6.81(1H, d, J=3.6 Hz),7.31–7.33(2H, m), 7.38(1H, t, J=1.8 Hz). IR(CHCl₃): 3516, 3450, 3431,2663, 1739, 1709, 1643, 1545, 1506 cm⁻¹. [α]_(D) ²¹+46.5±0.9°(c=1.002,MeOH) Anal. (C₂₆H₃₃NO₄S.0.1H₂O) Calcd.(%): C, 68.27; H, 7.32; N, 3.06;S, 7.01. Found(%): C, 68.08; H, 7.14; N, 3.21; S, 7.19.

Compound Number II-135

¹H-NMR(CDCl₃) δ: 0.94(1H, d, J=10.2 Hz), 1.09 and 1.21(each 3H, each s),1.50–2.42(14H, m), 4.20(1H, m), 4.41(2H, s), 5.33–5.49(2H, m), 6.01(1H,d, J=8.7 Hz), 6.91(1H, d, J=3.6 Hz), 7.11(1H, s), 7.27–7.35(3H, m),7.68–7.77(2H, m). IR(CHCl₃): 3512, 3446, 3431, 1709, 1645, 1543, 1508cm⁻¹. [α]_(D) ²⁴+44.9±0.9°(c=1.002, MeOH) Anal. (C₃₀H₃₅NO₃S₂.0.3H₂O)Calcd.(%): C, 68.35; H, 6.81; N, 2.66; S, 12.17. Found(%): C, 68.17; H,6.52; N, 2.68; S, 12.04.

Compound Number II-136

¹H-NMR(CDCl₃) δ: 0.94(1H, d, J=10.5 Hz), 1.09 and 1.21(each 3H, each s),1.50–2.41(14H, m), 4.19(1H, m), 4.29(2H, s), 5.33–5.48(2H, m), 6.02(1H,d, J=8.4 Hz), 6.51(1H, s), 6.91(1H, d, J=3.6 Hz), 7.16–7.25 (2H, m),7.34(1H, d, J=3.6 Hz), 7.42(1H, d, J=8.4 Hz), 7.50(1H, m). IR(CHCl₃):3516, 3450, 3431, 1739, 1709, 1643, 1545, 1508, 1454 cm⁻¹. [α]_(D)²³+42.3±0.8°(c=1.001, MeOH) Anal. (C₃₀H₃₅NO₄S.0.3H₂O) Calcd.(%): C,70.50; H, 7.02; N, 2.74; S, 6.27. Found(%): C, 70.36; H, 6.94; N, 2.70;S, 6.17.

Compound Number II-138

¹H-NMR(CDCl₃) δ: 0.94(1H, d, J=10.2 Hz), 1.08 and 1.20(each 3H, each s),1.49–2.42(14H, m), 4.20(1H, m), 4.19(2H, s), 5.33–5.48(2H, m), 5.99(1H,d, J=9.0 Hz), 6.80(1H, d, J=3.6 Hz), 7.22 (1H, d, J=7.5 Hz),7.31–7.50(7H, m), 7.57(2H, m). IR(CHCl₃): 3518, 3450, 3431, 2671, 1739,1709, 1643, 1543, 1506, 1471, 1456 cm⁻¹. [α]_(D) ²⁴+38.7±0.8°(c=1.014,MeOH) Anal. (C₃₄H₃₉NO₃S.0.2H₂O) Calcd.(%): C, 74.88; H, 7.28; N, 2.57;S, 5.88. Found(%): C, 74.92; H, 7.30; N, 2.75; S, 5.99.

Compound Number II-139

¹H-NMR(CDCl₃) δ: 0.97(1H, d, J=10.2 Hz), 1.06 and 1.22(each 3H, eachs),1.52–2.48(14H, m), 4.11(2H, s), 4.31(1H, m), 5.34–5.51(2H, m),6.15(1H, d, J=9.0 Hz), 7.19–7.30(6H, m), 7.76(1H, d, J=8.1 Hz), 7.83(1H,s), 8.15(1H, s) IR(CHCl₃): 3516, 3442, 2667, 1739, 1709, 1651, 1514,1495, 1471, 1454, 1435 cm⁻¹. [α]_(D) ²⁴+42.8±0.8°(c=1.011, MeOH) Anal.(C₃₂H₃₇NO₃S) Calcd.(%): C, 74.53; H, 7.23; N, 2.72; S, 6.22. Found(%):C, 74.25; H, 7.20; N, 2.97; S, 6.05.

Compound Number II-140

¹H-NMR(CDCl₃) δ: 0.98(1H, d, J=10.2 Hz), 1.10 and 1.23(each 3H, eachs),1.52–2.49(14H, m), 4.10(2H, s), 4.32(1H, m), 5.35–5.53(2H, m),6.17(1H, d, J=8.7 Hz), 7.19–7.32(6H, m), 7.64(1H, d, J=0.9 Hz), 7.76(1H,s), 8.21(1H, d, J=8.4 Hz). IR(CHCl₃): 3518, 3442, 2671, 1739, 1707,1651, 1514, 1493, 1469, 1454, 1404 cm⁻¹. [α]_(D) ²⁴+47.1±0.9°(c=1.001,MeOH) Anal. (C₃₂H₃₇NO₃S.0.2H₂O) Calcd.(%): C, 74.01; H, 7.26; N, 2.70;S, 6.17. Found(%): C, 73.89; H, 7.44; N, 2.93; S, 6.04.

Compound Number II-141

mp.134–135° C. 300 MHz ¹H-NMR(CDCl₃) δ: 0.93(1H, d, J=10.5 Hz), 0.98 and1.15(each 3H, each s),1.48–2.43(14H, m), 4.20(1H, m), 4.40 and 4.54(each1H, each d, J=16.5 Hz), 5.33–5.50(2H, m), 6.04(1H, d, J=8.4 Hz),6.99–7.30(6H, m), 7.55(1H, s), 7.73(1H, d, J=8.4 Hz). IR(CHCl₃): 3518,3437, 2669, 1741, 1709, 1653, 1510, 1471, 1454 cm⁻¹. [α]_(D)²⁵+54.2±0.9°(c=1.003, MeOH) Anal. (C₃₂H₃₇NO₃S.0.1H₂O) Calcd.(%): C,74.27; H, 7.25; N, 2.71; S, 6.20. Found(%): C, 74.11; H, 7.16; N, 3.15;S, 6.25.

Compound Number II-142

¹H-NMR(CDCl₃) δ: 0.94(1H, d, J=10.5 Hz), 1.08 and 1.21(each 3H, eachs),1.49–2.43(14H, m), 3.94(2H, s), 4.22(1H, m), 5.33–5.49(2H, m),6.03(1H, d, J=8.7 Hz), 7.04(1H, s), 7.17–7.33(6H, m). IR(CHCl₃): 3516,3448, 3433, 2669, 1739, 1709, 1645, 1549, 1508, 1471, 1454 cm⁻¹. [α]_(D)²⁵+40.5±0.8°(c=1.003, MeOH) Anal. (C₂₈H₃₅NO₃S.0.1H₂O) Calcd.(%): C,71.95; H, 7.59; N, 3.00; S, 6.86. Found(%): C, 71.82; H, 7.49; N, 3.37;S, 6.83.

Compound Number II-143

¹H-NMR(CDCl₃) δ: 0.98(1H, d, J=10.5 Hz), 1.10 and 1.23(each 3H, eachs),1.53–2.50(14H, m), 4.24(2H, s), 4.33(1H, m), 5.35–5.54(2H, m),6.18(1H, d, J=8.4 Hz), 7.19–7.30(6H, m), 7.42(1H, t, J=7.8 Hz), 7.78(1H,s), 8.18(1H, d, J=7.8 Hz). IR(CHCl₃): 3514, 3442, 2671, 1709, 1651,1516, 1495, 1471, 1454, cm⁻¹. [α]_(D) ²⁵+53.6±0.9°(c=1.003, MeOH), Anal.(C₃₂H₃₇NO₃S.0.1H₂O) Calcd.(%): C, 74.27; H, 7.25; N, 2.71; S, 6.20.Found(%): C, 74.18; H, 7.24; N, 2.90; S, 6.14.

Compound Number II-147

mp.117–118° C. 300 MHz ¹H-NMR(CDCl₃) δ: 0.94(1H, d, J=9.9 Hz), 1.09 and1.21(each 3H, each s), 1.55–2.42(14H, m), 3.87(3H, s), 4.06 (2H, s),4.18(1H, m), 5.35–5.49(2H, m), 5,56(1H, brs), 5.89(1H, d, J=8.7 Hz),6.72–6.77(3H, m), 6.87(1H, d, J=8.1 Hz), 7.31(1H, d, J=3.6 Hz).IR(Nujol): 3373, 3184, 2667, 1705, 1622, 1599, 1547, 1520, 1286 cm⁻¹.[α]_(D) ²³+42.0±0.8°(c=1.008, MeOH) Anal. (C₂₉H₃₇NO₅S) Calcd.(%): C,68.07; H, 7.29; N, 2.74; S, 6.27. Found(%): C, 67.84; H, 7.43; N, 2.71;S, 6.18.

Compound Number II-148

¹H-NMR(CDCl₃) δ: 0.95(1H, d, J=9.9 Hz), 1.10 and 1.23(each 3H, each s),1.53–2.45(14H, m), 3.87(3H, s), 2.96–3.01(2H, m), 3.10–3.16(2H, m),4.22(1H, m), 5.34–5.50(2H, m), 6.01(1H, d, J=8.4 Hz), 6.71(1H, d, J=3.9Hz), 7.16–7.32(6H, m). IR(CHCl₃): 3518, 3450, 3431, 2671, 1739, 1709,1641, 1545, 1508 cm⁻¹. [α]_(D) ²²+44.3±0.8°(c=1.006, MeOH) Anal.(C₂₉H₃₇NO₃S.0.1H₂O) Calcd.(%): C, 72.34; H, 7.79; N, 2.91; S, 6.66.Found(%): C, 72.24; H, 7.68; N, 3.11; S, 6.73.

Compound Number II-149

¹H-NMR(CDCl₃) δ: 0.95(1H, d, J=10.2 Hz), 1.10 and 1.23(each 3H, each s),1.52–2.45(14H, m), 2.43(3H, d, J=0.9 Hz), 3.07–3.18(4H, m), 4.21(1H, m),5.35–5.50(2H, m), 6.02(1H, d, J=8.4 Hz), 6.53–6.57(2H, m), 6.76 and7.30(each 1H, each d, each J=3.9 Hz). IR(CHCl₃): 3516, 3450, 3431, 2667,1709, 1641, 1543, 1508 cm⁻¹. [α]_(D) ²²+43.1±0.8°(c=1.005, MeOH) Anal.(C₂₈H₃₇NO₃S₂.0.3H₂O) Calcd.(%): C, 66.58; H, 7.50; N, 2.77; S, 12.70.Found(%): C, 66.47; H, 7.46; N, 2.99; S, 12.62.

Compound Number II-150

¹H-NMR(CDCl₃) δ: 0.95(1H, d, J=10.2 Hz), 1.10 and 1.23(each 3H, each s),1.52–2.45(14H, m), 3.19(4H, s), 4.21(1H, m), 5.34–5.50(2H, m), 6.01(1H,d, J=8.4 Hz), 6.75(1H, d, J=3.9 Hz), 6.79(1H, m), 6.91 (1H, dd, J=3.6and 5.1 Hz), 7.13(1H, dd, J=0.9 and 5.1 Hz), 7.29(1H, d, J=3.9 Hz).IR(CHCl₃): 3514, 3450, 3433, 2667,n 1739, 1709, 1641, 1545, 1508 cm⁻¹.[α]_(D) ²⁴+33.5±0.8°(c=1.009, MeOH) Anal. (C₂₇H₃₅NO₃S₂) Calcd.(%): C,66.77; H, 7.26; N, 2.88; S, 13.20. Found(%): C, 66.48; H, 7.31; N, 2.97;S, 13.22.

Compound Number II-151

¹H-NMR(CDCl₃) δ: 0.97(1H, d, J=9.9 Hz), 1.12 and 1.23(each 3H, each s),1.53–2.47(14H, m), 3.00–3.06(2H, m), 3.12–3.17(2H, m), 4.27 (1H, m),5.34–5.51(2H, m), 6.24(1H, d, J=9.0 Hz), 6.75(1H, m), 6.90(1H, dd, J=3.6and 5.4 Hz), 7.12(1H, dd, J=1.2 and 5.4 Hz), 7.25 and 7.64(each 2H, eachd-like). IR(CHCl₃): 3516, 3452, 2665, 1738, 1709, 1649, 1523, 1495 cm⁻¹.[α]_(D) ²⁴+54.5±0.9°(c=1.016, MeOH) Anal. (C₂₉H₃₇NO₃S) Calcd.(%): C,72.61; H, 7.77; N, 2.92; S, 6.68. Found(%): C, 72.51; H, 7.69; N, 2.98;S, 6.62.

Compound Number II-152

¹H-NMR(CDCl₃) δ: 0.95(1H, d, J=10.2 Hz), 1.10 and 1.23(each 3H, each s),1.51–2.45(14H, m), 2.92–2.97(2H, m), 3.08–3.13(2H, m), 4.22 (1H, m),5.34–5.50(2H, m), 6.00(1H, d, J=8.7 Hz), 6.69(1H, d, J=3.6 Hz),6.92–7.00 (2H, m), 7.09–7.15(2H, m), 7.28(1H, d, J=3.6 Hz). IR(CHCl₃):3516, 3450, 3431, 1741, 1709, 1641, 1543, 1510, 1471 cm⁻¹. [α]_(D)²³+42.6±0.8°(c=1.014, MeOH) Anal. (C₂₉H₃₆FNO₃S) Calcd.(%): C, 69.99; H,7.29; N, 2.81; S, 6.44; F, 3.82. Found(%): C, 69.87; H, 7.29; N, 2.88;S, 6.50; F, 3.85.

Compound Number II-156

mp.93–95° C. ¹H-NMR(CDCl₃) δ: 0.96(1H, d, J=10.2 Hz), 1.13 and 1.23(each3H, each s), 1.52–2.47(14H, m), 4.08(2H, s), 4.27(1H, m), 5.34–5.51(2H,m), 6.21(1H, d, J=8.7 Hz), 7.18–7.32(6H, m), 7.61 and 7.66(each 1H, eachs), 7.74(1H, d, J=8.4 Hz). IR(KBr): 3367, 1705, 1618, 1556, 1533, 1508cm⁻¹. [α]_(D) ²³+60.4±0.8°(c=1.012, MeOH) Anal. (C₃₂H₃₇NO₃S) Calcd.(%):C, 74.53; H, 7.23; N, 2.72; S, 6.22. Found(%): C, 74.31; H, 7.37; N,2.99; S, 6.10.

Compound Number II-157

¹H-NMR(CDCl₃) δ: 0.92(1H, d, J=10.2 Hz), 1.06 and 1.19(each 3H, each s),1.47–2.42(14H, m), 4.20(1H, m), 4.28(2H, s), 5.32–5.47(2H, m), 5.98(1H,d, J=8.7 Hz), 6.80(1H, d, J=3.3 Hz), 7.32–7.36(2H, m), 7.41–7.50(2H, m),7.68(1H, s), 7.77–7.83(3H, m). IR(CHCl₃): 3518, 3450, 3431, 1739, 1709,1641, 1545, 1508, 1471 cm⁻¹. [α]_(D) ²³+42.7±0.8°(c=1.003, MeOH) Anal.(C₃₂H₃₇NO₃S.0.2H₂O) Calcd.(%): C, 74.01; H, 7.26; N, 2.70; S, 6.17.Found(%): C, 73.94; H, 7.30; N, 2.89; S, 6.15.

Compound Number II-158

¹H-NMR(CDCl₃) δ: 0.95(1H, d, J=10.5 Hz), 1.11 and 1.22(each 3H, each s),1.51–2.45(14H, m), 2.94–3.00(2H, m), 3.06–3.12(2H, m), 3.83 (3H, s),4.22(1H, m), 5.34–5.50(2H, m), 6.00(1H, d, J=8.7 Hz), 6.73 (1H, d, J=3.6Hz), 6.84–6.89(2H, m), 7.09(1H, dd, J=1.5 and 7.8 Hz), 7.20 (1H, dt,J=1.5 and 7.8 Hz), 7.30(1H, d, J=3.6 Hz). IR(CHCl₃): 3518, 3450, 3431,1741, 1709, 1639, 1545, 1506, 1496, 1466 cm⁻¹. [α]_(D)²⁵+41.3±0.8°(c=1.007, MeOH) Anal. (C₃₀H₃₉FNO₄S) Calcd.(%): C, 70.69; H,7.71; N, 2.75; S, 6.29. Found(%): C, 70.42; H, 7.64; N, 2.78; S, 6.37.

Compound Number II-159

¹H-NMR(CDCl₃) δ: 0.94(1H, d, J=10.2 Hz), 1.10 and 1.22(each 3H, each s),1.53–2.48(14H, m), 2.96–3.04(2H, m), 3.07–3.16(2H, m), 4.22 (1H, m),5.34–5.52(2H, m), 6.04(1H, d, J=8.7 Hz), 6.74(1H, d, J=3.6 Hz),6.77–6.85 (2H, m), 7.05–7.11 (2H, m), 7.31(1H, d, J=3.6 Hz). IR(CHCl₃):359, 3510, 3429, 3190, 1709, 1636, 1545, 1508, 1456 cm⁻¹. [α]_(D)²⁵+42.7±0.8°(c=1.009, MeOH) Anal. (C₂₉H₃₇NO₄S.0.3H₂O) Calcd.(%): C,69.51; H, 7.56; N, 2.80; S, 6.40. Found(%): C, 69.25; H, 7.43; N, 2.89;S, 6.43.

Compound Number II-160

mp.125–126° C. 300 MHz ¹H-NMR(CDCl₃) δ: 0.96(1H, d, J=10.2 Hz), 1.13 and1.23(each 3H, each s), 1.52–2.47(14H, m), 4.10(2H, s), 4.27 (1H, m),5.34–5.51(2H, m), 6.20(1H, d, J=9.0 Hz), 7.19–7.33(6H, m), 7.62 and7.69(each 1H, each s), 7.73(1H, d, J=8.4 Hz). IR(KBr): 3415, 3199, 1736,1703, 1633, 1523 cm⁻¹. [α]_(D) ²⁵+53.3±0.8°(c=1.002, MeOH) Anal.(C₃₂H₃₇NO₃S.0.1H₂O) Calcd.(%): C, 74.27; H, 7.25; N, 2.71; S, 6.23.Found(%): C, 74.19; H, 7.16; N, 2.81; S, 6.23.

Compound Number II-161

mp.98–101° C. ¹H-NMR(CDCl₃) δ: 0.97(1H, d, J=10.5 Hz), 1.14 and1.24(each 3H, each s), 1.53–2.47(14H, m), 4.08(2H, s), 4.27 (1H, m),5.35–5.51(2H, m), 6.21(1H, d, J=8.7 Hz), 6.90(1H, dd, J=1.2 and 5.1 Hz),6.93(1H, m), 7.24–7.29(2H, m), 7.63(1H, s), 7.75(1H, d, J=8.1 Hz).IR(KBr): 3394, 3097, 1707, 1643, 1533, 1500 cm⁻¹. [α]_(D)²⁵+58.7±1.0°(c=1.006, MeOH) Anal. (C₃₀H₃₅NO₃S₂.0.3H₂O) Calcd.(%): C,68.35; H, 6.81; N, 2.66; S, 12.17. Found(%): C, 68.27; H, 6.76; N, 2.94;S, 12.17.

Compound Number II-162

mp.106–109° C. ¹H-NMR(CDCl₃) δ: 0.97(1H, d, J=10.2 Hz), 1.14 and1.24(each 3H, each s), 1.53–2.47(14H, m), 4.26(2H, s), 4.27(1H, m),5.35–5.51(2H, m), 6.22(1H, d, J=8.7 Hz), 6.82(1H, m), 6.93(1H, dd, J=3.6and 5.1 Hz), 7.16(1H, dd, J=1.2 and 5.1 Hz), 7.32(1H, dd, J=8.1 and 1.8Hz), 7.68(2H, m), 7.76(1H, d, J=8.1 Hz). IR(KBr): 3396, 3070, 1707,1645, 1535, 1500 cm⁻¹. [α]_(D) ²⁵+59.9±1.0°(c=1.005, MeOH) Anal.(C₃₀H₃₅NO₃S₂.0.2H₂O) Calcd.(%): C, 68.59; H, 6.79; N, 2.67; S, 12.21.Found(%): C, 68.57; H, 6.62; N, 2.76; S, 12.17.

Compound Number II-163

¹H-NMR(CDCl₃) δ: 0.94(1H, d, J=10.2 Hz), 1.09 and 1.22(each 3H, each s),1.49–2.44(14H, m), 4.12(2H, s), 4.23(1H, m), 5.34–5.49(2H, m), 6.09(1H,d, J=8.7 Hz), 6.82 and 6.93(each 1H, each m), 7.13–7.17 (2H, m),7.34(1H, d, J=1.5 Hz). IR(CHCl₁₃): 3512, 3448, 3431, 1739, 1709, 1645,1550, 1508, 1471, 1456 cm⁻¹. [α]_(D) ²⁵+43.3±0.8°(c=1.007, MeOH) Anal.(C₂₆H₃₃NO₃S₂.0.1H₂O) Calcd.(%): C, 65.95; H, 7.07; N, 2.96; S, 13.54.Found(%): C, 66.12; H, 7.06; N, 3.04; S, 13.66.

Compound Number II-164

¹H-NMR(CDCl₃) δ: 0.94(1H, d, J=10.5 Hz), 1.09 and 1.22 (each 3H, eachs), 1.49–2.44(14H, m), 3.95(2H, s), 4.22(1H, m), 5.34–5.49 (2H, m),6.06(1H, d, J=8.7 Hz), 6.92 and 6.96(each 1H, each m), 7.07(1H, d, J=1.5Hz), 7.28(1H, m), 7.30(1H, d, J=1.5 Hz). IR(CHCl₃): 3510, 3431, 1739,1709, 1645, 1550, 1508, 1471 cm⁻¹. [α]_(D) ²⁵+41.1±0.8°(c=1.009, MeOH)Anal. (C₂₆H₃₃NO₃S₂.0.2H₂O) Calcd.(%): C, 65.70; H, 7.08; N, 2.95; S,13.49. Found(%): C, 65.57; H, 6.97; N, 3.08; S, 13.63.

Compound Number II-165

¹H-NMR(CDCl₃) δ: 0.95(1H, d, J=10.2 Hz), 1.10 and 1.22(each 3H, each s),1.50–2.44(14H, m), 3.74(2H, s), 4.23(1H, m), 5.34–5.50(2H, m), 6.07(1H,d, J=8.0 Hz), 6.23(1H, s), 7.08(1H, d, J=1.5 Hz), 7.24(1H, s), 7.31(1H,d, J=1.5 Hz), 7.36(1H, m). IR(CHCl₃): 3510, 3448, 3431, 2663, 1709,1645, 1550, 1508, 1471 cm⁻¹. [α]_(D) ²⁵+44.2±0.8°(c=1.001, MeOH) Anal.(C₂₆H₃₃NO₄S.0.2H₂O) Calcd.(%): C, 68.00; H, 7.33; N, 3.05; S, 6.98.Found(%): C, 68.00; H, 7.30; N, 3.15; S, 7.12.

Compound Number II-166

¹H-NMR(CDCl₃) δ: 0.92(1H, d, J=10.2 Hz), 1.05 and 1.19(each 3H, each s),1.48–2.40(14H, m), 4.17(1H, m), 4.58(2H, s), 5.31–5.46(2H, m), 5.96(1H,d, J=8.7 Hz), 6.72 and 7.26(each 1H, each d, each J=3.9 Hz),7.37–7.51(4H, m), 7.79(1H, d, J=8.1 Hz), 7.87 and 7.97 (each 1H, eachm). IR(CHCl₃): 3516, 3450, 3431, 2667, 1739, 1709, 1641, 1543, 1508,1471 cm⁻¹. [α]_(D) ^(25.5)+41.9±0.8°(c=1.011, MeOH) Anal.(C₃₂H₃₇NO₃S.0.2H₂O) Calcd.(%): C, 74.01; H, 7.26; N, 2.70; S, 6.17.Found(%): C, 74.10; H, 7.13; N, 2.99; S, 6.15.

Compound Number II-167

¹H-NMR(CDCl₃) δ: 0.93(1H, d, J=10.2 Hz), 1.05 and 1.20(each 3H, each s),1.48–2.42(14H, m), 4.20(1H, m), 4.39(2H, m), 5.31–5.46(2H, m), 6.00(1H,d, J=9.0 Hz), 6.96(1H, s), 7.30–7.33(2H, m), 7.40–7.50 (3H, m), 7.78(1H,d, J=8.1 Hz), 7.87 and 7.95(each 1H, each m). IR(CHCl₃): 3518, 3448,3431, 2665, 1738, 1709, 1645, 1549, 1508, 1471 cm⁻¹. [α]_(D)²⁴+37.9±0.8°(c=1.004, MeOH) Anal. (C₃₂H₃₇NO₃S.0.1H₂O) Calcd.(%): C,74.27; H, 7.25; N, 2.71; S, 6.20. Found(%): C, 74.13; H, 7.18; N, 2.87;S, 6.26.

Compound Number II-169

¹H-NMR(CDCl₃) δ: 0.98(1H, d, J=10.5 Hz), 1.10 and 1.23(each 3H, eachs),1.53–2.50(14H, m), 4.23(2H, s), 4.33(1H, m), 5.35–5.54(2H, m),6.18(1H, d, J=8.7 Hz), 6.92(1H, dd, J=1.2 and 4.8 Hz), 7.01(1H, m),7.22(1H, d, J=7.8 Hz), 7.24(1H, dd, J=3.0 and 4.8 Hz), 7.42(1H, d, J=7.8and 8.1 Hz), 7.79(1H, s), 8.18(1H, d, J=8.1 Hz). IR(CHCl₃): 3516, 3442,2667, 1709, 1651, 1516, 1495, 1471 cm⁻¹. [α]_(D) ²⁶+50.9±0.9°(c=1.009,MeOH), Anal. (C₃₀H₃₅NO₃S₂.0.2H₂O) Calcd.(%): C, 68.59; H, 6.79; N, 2.67;S, 12.21. Found(%): C, 68.51; H, 6.69; N, 2.73; S, 12.39.

Compound Number II-170

¹H-NMR(CDCl₃) δ: 0.99(1H, d, J=10.2 Hz), 1.11 and 1.24(each 3H, each s),1.53–2.50(14H, m), 4.03(2H, s), 4.34(1H, m), 5.36–5.54 (2H, m), 6.20(1H,d, J=8.4 Hz), 7.24(1H, d, J=8.4 Hz), 7.24(1H, d, J=7.2 Hz), 7.30(1H, m),7.35(1H, t, J=1.8 Hz), 7.42(1H, dd, J=7.2 and 8.1 Hz), 7.81(1H, s),8.19(1H, d, J=7.2 Hz). IR(CHCl₃): 3518, 3442, 1739, 1709, 1651, 1516,1496, 1471 cm⁻¹. [α]_(D) ²⁵+54.3±1.0°(c=1.002, MeOH) Anal.(C₃₀H₃₅NO₄S.0.1H₂O) Calcd.(%): C, 71.00; H, 6.99; N, 2.76; S, 6.32.Found(%): C, 70.95; H, 6.82; N, 2.74; S, 6.35.

Compound Number II-173

¹H-NMR(CDCl₃) δ: 0.99(1H, d, J=10.5 Hz), 1.16 and 1.24(each 3H, each s),1.53–2.48(14H, m), 3.93(2H, s), 4.32(1H, m), 5.34–5.52(2H, m), 6.35(1H,d, J=8.7 Hz), 7.31–7.42(2H, m), 7.56(1H, d, J=6.9 Hz), 7.71(1H, dd,J=1.5 and 8.1 Hz), 7.78–7.83(2H, m), 7.92(1H, s). IR (CHCl₃): 3516,3452, 3026, 2667, 1738, 1709, 1649, 1641, 1514, 1481, 1469, 1454 cm⁻¹.[α]_(D) ²⁴+67.5±1.1°(c=1.005, MeOH) Anal. (C₃₀H₃₅NO₃.0.1H₂O) Calcd.(%):C, 78.43; H, 7.72; N, 3.05. Found(%): C, 78.36; H, 7.99; N, 3.24.

Compound Number II-174

¹H-NMR(CDCl₃) δ: 0.93(1H, d, J=10.2 Hz), 1.09 and 1.21(each 3H, eachs),1.50–2.42(14H, m), 3.21(2H, t, J=8.7 Hz), 4.02(2H, s), 4.20 (1H, m),4.59(2H, t, J=8.7 Hz), 5.34–5.49(2H, m), 6.01(1H, d, J=8.7 Hz), 6.80(1H, d, J=3.6 Hz), 7.06(1H, d, J=1.8 Hz), 7.19(1H, m), 7.30 (1H, d,J=3.6 Hz). IR(CHCl₃): 3512, 3450, 3431, 2667, 1739, 1709, 1641, 1543,1508, 1460 cm⁻¹. [α]_(D) ²⁵+35.7±0.8°(c=1.002, MeOH), Anal.(C₃₀H₃₆BrNO₄S) Calcd.(%): C, 61.43; H, 6.19; Br, 13.62; N, 2.39; S,5.47. Found(%): C, 61.26; H, 6.11; Br, 13.54; N, 2.46; S, 5.47.

Compound Number II-175

¹H-NMR(CDCl₃) δ: 0.96(1H, d, J=10.2 Hz), 1.14 and 1.23(each 3H, eachs),1.52–2.46(14H, m), 4.21((2H, s), 4.28(1H, m), 5.34–5.51(2H, m),6.23(1H, d, J=9.0 Hz), 6.94(1H, dd, J=1.2 and 4.8 Hz), 7.05(1H, m),7.21–7.26(2H, m), 7.35(1H, dd, J=7.5 and 8.1 Hz), 7.71(1H, d, J=7.5 Hz),7.75(1H, s). IR(CHCl₃): 3510, 3448, 3427, 2665, 1709, 1649, 1539, 1504,1469, 1454 cm⁻¹. [α]_(D) ²⁵+47.4±0.9°(c=1.005, MeOH), Anal.(C₃₂H₃₇NO₃S.0.1H₂O) Calcd.(%): C, 74.27; H, 7.25; N, 2.71; S, 6.20.Found(%): C, 74.15; H, 7.14; N, 2.89; S, 6.26.

Compound Number II-176

¹H-NMR(CDCl₃) δ: 0.97(1H, d, J=10.2 Hz), 1.14 and 1.24(each 3H, each s),1.53–2.47(14H, m), 4.22((2H, s), 4.27(1H, m), 5.35–5.51(2H, m), 6.22(1H,d, J=8.7 Hz), 6.94(1H, dd, J=1.2 and 4.8 Hz), 7.05(1H, m), 7.21–7.26(2H,m), 7.35(1H, dd, J=7.5 and 8.1 Hz), 7.71(1H, d, J=7.5 Hz), 7.75(1H, s).IR(CHCl₃): 3512, 3448, 3427, 2665, 1709, 1649, 1539, 1504, 1469 cm⁻¹.[α]_(D) ²⁵+46.1±0.9°(c=1.011, MeOH), Anal. (C₃₀H₃₅NO₃S₂) Calcd.(%): C,69.06; H, 6.76; N, 2.68; S, 12.29. Found(%): C, 68.77; H, 6.84; N, 2.78;S, 12.30.

Compound Number II-177

¹H-NMR(CDCl₃) δ: 0.96(1H, d, J=10.2 Hz), 1.14 and 1.24(each 3H, eachs),1.53–2.46(14H, m), 2.31(3H, s), 4.17((2H, s), 4.28(1H, m), 5.34–5.51(2H, m), 6.22(1H, d, J=9.0 Hz), 7.09 and 7.15(each 2H, each d, J=7.8Hz), 7.19(1H, d, J=7.2 Hz), 7.34(1H, dd, J=7.2 and 7.8 Hz), 7.70 (1H, d,J=7.8 Hz), 7.75(1H, s). IR(CHCl₃): 3510, 3448, 3427, 2669, 1709, 1649,1537, 1504, 1469 cm⁻¹. [α]_(D) ²⁵+45.6±0.9°(c=1.005, MeOH), Anal.(C₃₃H₃₉NO₃S.0.1H₂O) Calcd.(%): C, 74.57; H, 7.43; N, 2.64; S, 6.03.Found(%): C, 74.46; H, 7.48; N, 2.78; S, 6.15.

Compound Number II-178

¹H-NMR(CDCl₃) δ: 0.97(1H, d, J=10.2 Hz), 1.14 and 1.24(each 3H, eachs),1.53–2.47(14H, m), 2.31(3H, s), 4.28(1H, m), 4.40((2H, s), 5.35–5.51(2H, m), 6.23(1H, d, J=8.7 Hz), 6.92–6.94(2H, m), 7.16(1H, dd, J=1.5 and5.1 Hz), 7.28(1H, d, J=7.5 Hz), 7.36(1H, t, J=7.5 Hz), 7.72 (1H, d,J=7.5 Hz), 7.75(1H, s). IR(CHCl₃): 3508, 3448, 3427, 2663, 1709, 1649,1539, 1504, 1469 cm⁻¹. [α]_(D) ²⁵+46.2±0.9°(c=1.005, MeOH), Anal.(C₃₀H₃₅NO₃S₂) Calcd.(%): C, 69.06; H, 6.76; N, 2.68; S, 12.29. Found(%):C, 68.84; H, 6.86; N, 2.79; S, 12.28.

Compound Number II-179

¹H-NMR(CDCl₃) δ: 0.94(1H, d, J=10.5 Hz), 1.08 and 1.21(each 3H, each s),1.51–2.42(14H, m), 4.09(2H, s), 4.18(1H, m), 5.33–5.48(2H, m), 5.96(1H,d, J=9.3 Hz), 6.54(1H, d, J=3.6 Hz), 7.24–7.42(10H, m). IR(CHCl₃): 3510,3450, 3431, 1739, 1709, 1641, 1543, 1506, 1479, 1458 cm⁻¹. [α]_(D)^(24.5)+39.4±0.8°(c=1.007, MeOH) Anal. (C₃₄H₃₉NO₃S.0.1H₂O) Calcd.(%): C,75.13; H, 7.27; N, 2.58; S, 5.90. Found(%): C, 75.05; H, 7.32; N, 2.69;S, 6.17.

Compound Number II-180

¹H-NMR(CDCl₃) δ: 1.00(1H, d, J=10.2 Hz), 1.15 and 1.26(each 3H, each s),1.55–2.49(14H, m), 4.30(1H, m), 5.37–5.53(2H, m), 6.38(1H, d, J=8.1 Hz),7.32(1H, m), 7.49–7.58(3H, m), 7.64–7.67(2H, m), 7.92 (1H, s).IR(CHCl₃): 3514, 3446, 1714, 1655, 1618, 1514, 1469, 1446 cm⁻¹. [α]_(D)²⁵+66.7±1.1°(c=1.005, MeOH) Anal. (C₃₀H₃₃NO₄.0.2H₂O) Calcd.(%): C,75.83; H, 7.08; N, 2.95. Found(%): C, 75.69; H, 7.05; N, 3.08.

Compound Number II-181

mp.103–104° C. 300 MHz ¹H-NMR(CDCl₃) δ: 0.93(1H, d, J=10.2 Hz), 1.08 and1.21(each 3H, each s),1.49–2.42(14H, m), 3.79(3H, s), 4.07 ((2H, s),4.20(1H, m), 5.33–5.48(2H, m), 5.98(1H, d, J=8.7 Hz), 6.75 (1H, d, J=3.6Hz), 6.85 and 7.15(each 2H, each d, J=8.4 Hz), 7.31 (1H, d, J=3.6 Hz).IR(CHCl₃): 3519, 3450, 3431, 1741, 1709, 1641, 1612, 1543, 1510, 1464cm⁻¹. [α]_(D) ²⁵+43.8±0.8°(c=1.009, MeOH) Anal. (C₂₉H₃₇NO₄S) Calcd.(%):C, 70.27; H, 7.52; N, 2.83; S, 6.47. Found(%): C, 70.33; H, 7.55; N,3.05; S, 6.46.

Compound Number II-182

¹H-NMR(CDCl₃) δ: 0.93(1H, d, J=10.5 Hz), 1.07 and 1.21(each 3H, eachs),1.49–2.42(14H, m), 4.20(1H, m), 4.37(2H, s), 5.33–5.48(2H, m),5.99(1H, d, J=8.4 Hz), 6.82(1H, d, J=3.6 Hz), 7.21(1H, s), 7.30 (1H, d,J=3.6 Hz), 7.34–7.37(2H, m), 7.69(1H, m), 7.86(1H, m). IR (CHCl₃): 3512,3450, 3431, 2671, 1739, 1709, 1643, 1543, 1508, 1471, 1460 cm⁻¹. [α]_(D)²⁵+40.2±0.8°(c=1.005, MeOH), Anal. (C₃₀H₃₅NO₃S₂.0.4H₂O) Calcd.(%): C,68.12; H, 6.82; N, 2.64; S, 12.12. Found(%): C, 68.05; H, 6.70; N, 2.87;S, 12.00.

Compound Number II-183

¹H-NMR(CDCl₃) δ: 0.93(1H, d, J=10.2 Hz), 1.08 and 1.21(each 3H, each s),1.50–2.47(14H, m), 4.13(2H, s), 4.20(1H, m), 5.33–5.50(2H, m), 6.01(1H,d, J=9.0 Hz), 6.80(1H, m), 6.82(1H, m), 6.86(1H, m), 7.12 (1H, m),7.15(1H, m), 7.31(1H, d, J=3.9 Hz). IR(CHCl₃): 3597, 3510, 3448, 3427,3190, 1709, 1633, 1545, 1508, 1456 cm⁻¹. [α]_(D) ²⁴+41.8°±0.8°(c=1.004,MeOH) Anal. (C₂₈H₃₅NO₄S.0.3H₂O) Calcd.(%): C, 69.11; H, 7.37; N, 2.88;S, 6.59. Found(%): C, 68.94; H, 7.42; N, 2.96; S, 6.73.

Compound Number II-184

¹H-NMR(CDCl₃) δ: 1.00(1H, d, J=10.5 Hz), 1.17 and 1.25(each 3H, each s),1.55–2.50(14H, m), 3.93 (2H, s), 4.32(1H, m), 5.35–5.49(2H, m), 6.37(1H,d, J=8.7 Hz), 7.31–7.43(2H, m), 7.54–7.63(3H, m), 7.84 (1H, d, J=7.2Hz), 8.16(1H, s). IR (CDCl₃): 3514, 3450, 2667, 1709, 1651, 1572, 1514,1481, 1452 cm⁻¹. [α]_(D) ²⁴+58.3±1.0°(c=1.003, MeOH) Anal.(C₃₀H₃₅NO₃.0.1H₂O) Calcd.(%): C, 78.43; H, 7.72; N, 3.05. Found(%): C,78.26; H, 7.73; N, 3.28.

Compound Number II-185

¹H-NMR(CDCl₃) δ: 0.94(1H, d, J=10.2 Hz), 1.09 and 1.21(each 3H, each s),1.52–2.42(14H, m), 4.16(2H, s), 4.19(1H, m), 5.33–5.47(2H, m), 5.99(1H,d, J=9.3 Hz), 6.78(1H, d, J=3.6 Hz), 7.00–7.12(2H, m), 7.20–7.27 (2H,m), 7.30(1H, d, J=3.6 Hz). IR(CHCl₃): 3510, 3450, 3431, 1741, 1709,1643, 1543, 1508, 1456 cm⁻¹. [α]_(D) ²⁴+38.0±0.8°(c=1.03, CHCl₃) Anal.(C₂₈H₃₄FNO₃S.0.5H₂O) Calcd.(%): C, 68.26; H, 7.16; N, 2.86; S, 6.51; F,3.86. Found(%): C, 68.24; H, 7.08; N, 2.93; S, 6.50; F, 3.80.

Compound Number II-188

mp.53–55° C. 300 MHz ¹H-NMR(CDCl₃) δ: 0.94(1H, d, J=10.2 Hz), 1.08 and1.21(each 3H, each s),1.51–2.42(14H, m), 4.07(2H, s), 4.19 (1H, m),5.05(2H, s), 5.33–5.48(2H, m), 5.98(1H, d, J=9.0 Hz), 6.76 (1H, d, J=3.6Hz), 6.92 and 7.15(each 2H, each d, J=8.7 Hz), 7.31(1H, d, J=3.6 Hz),7.32.–7.43 (5H, m) IR(CHCl₃): 3518, 3450, 3431, 1741, 1709, 1641, 1612,1545, 1510, 1469, 1456 cm⁻¹. [α]_(D) ²⁴+36.0±0.8°(c=1.005, MeOH), Anal.(C₃₅H₄₁NO₄S.0.4H₂O) Calcd.(%): C, 72.61; H, 7.28; N, 2.42; S, 5.54.Found(%): C, 72.58; H, 7.33; N, 2.65; S, 5.53.

Compound Number II-189

300 MHz ¹H-NMR(CDCl₃) δ: 0.94(1H, d, J=10.5 Hz), 1.08 and 1.21 (each 3H,each s),1.51–2.42(14H, m), 4.07(2H, s), 4.19(1H, m), 4.51–4.53 (2H, m),5.26–5.46(4H, m), 5.98(1H, d, J=8.7 Hz), 6.05(1H, m), 6.76 (1H, d, J=3.6Hz), 6.87 and 7.14(each 2H, each d, J=8.7 Hz), 7.31 (1H, d, J=3.6 Hz).IR(CHCl₃): 3511, 3450, 3431, 1741, 1709, 1641, 1612, 1543, 1508, 1471,1458 cm⁻¹. [α]_(D) ²⁴+39.7±0.8°(c=1.008, MeOH), Anal.(C₃₁H₃₉NO₄S.0.2H₂O) Calcd.(%): C, 70.88; H, 7.56; N, 2.67; S, 6.10.Found(%): C, 70.86; H, 7.60; N, 2.68; S, 6.17.

Compound Number II-190

¹H-NMR(CDCl₃) δ: 0.94(1H, d, J=10.2 Hz), 1.09 and 1.21(each 3H, eachs),1.50–2.43(14H, m), 4.04(2H, s), 4.20(1H, m), 5.33–5.49(2H, m),5.94(2H, s), 5.98(1H, d, J=8.7 Hz), 6.68–6.78(4H, m), 7.31(1H, d, J=3.9Hz). IR(CHCl₃): 3518, 3450, 3431, 1739, 1709, 1641, 1543, 1504, 1489,1444, 1250, 1041 cm⁻¹. [α]_(D) ²⁴+42.2±0.8°(c=1.010, MeOH), Anal.(C₂₉H₃₅NO₅S) Calcd.(%): C, 68.34; H, 6.92; N, 2.75; S, 6.29. Found(%):C, 68.19; H, 6.88; N, 2.86; S, 6.20.

Compound Number II-191

mp.76–80° C. ¹H-NMR(CDCl₃) δ: 0.94(1H, d, J=9.9 Hz), 1.09 and 1.21 (each3H, each s),1.51–2.43(14H, m), 4.13(2H, s), 4.20(1H, m), 5.34–5.49(2H,m), 6.00(1H, d, J=8.4 Hz), 6.78(1H, d, J=3.9 Hz), 6.90–7.04 (3H, m),7.27(1H, m), 7.32(1H, d, J=3.9 Hz). IR(Nujol): 3408, 1703, 1631, 1514,1250 cm⁻¹. [α]_(D) ²⁵+51.0±0.9°(c=1.001, MeOH), Anal. (C₂₈H₃₄FNO₃S)Calcd.(%): C, 69.54; H, 7.09; N, 2.90; S, 6.63; F, 3.93. Found(%): C,69.77; H, 7.23; N, 2.95; S, 6.55; F, 3.93.

Compound Number II-192

¹H-NMR(CDCl₃) δ: 0.94(1H, d, J=10.2 Hz), 1.09 and 1.22(each 3H, eachs),1.51–2.44(14H, m), 4.19(2H, s), 4.20(1H, m), 5.34–5.49(2H, m),6.00(1H, d, J=8.4 Hz), 6.78 and 7.32(each 1H, each d, each J=3.6 Hz),7.40–7.54(4H, m). IR(CHCl₃): 3516, 3450, 3431, 1739, 1709, 1643, 1543,1508, 1331, 1167, 1130 cm⁻¹. [α]_(D) ²⁵+39.5±0.8°(c=1.012, MeOH), Anal.(C₂₉H₃₄F₃NO₃S) Calcd.(%): C, 65.27; H, 6.42; N, 2.62; S, 6.01; F, 10.68.Found(%): C, 65.05; H, 6.46; N, 2.74; S, 6.02; F, 10.63.

Compound Number II-193

¹H-NMR(CDCl₃) δ: 0.94(1H, d, J=10.2 Hz), 1.09 and 1.21(each 3H, each s),1.51–2.26(14H, m), 4.19(1H, m), 4.26(2H, s), 5.33–5.49(2H, m), 6.00(1H,d, J=8.4 Hz), 6.79(1H, d, J=3.9 Hz), 7.20–7.25(3H, m), 7.30(1H, d, J=3.9Hz), 7.37–7.40(1H, m). IR(CHCl₃): 3516, 3450, 3431, 1741, 1709, 1643,1543, 1508, 1471 cm⁻¹. [α]_(D) ²⁵+38.5±0.8°(c=1.00, CHCl₃) Anal.(C₂₈H₃₄FNO₃S.0.5H₂O) Calcd.(%): C, 66.06; H, 6.93; N, 2.75; S, 6.30; Cl,6.96. Found(%): C, 66.21; H, 6.87; N, 2.97; S, 6.24; Cl, 6.75.

Compound Number II-194

¹H-NMR(CDCl₃) δ: 0.93(1H, d, J=10.5 Hz), 1.07 and 1.20(each 3H, each s),1.49–2.42(14H, m), 2.30(6H, s), 4.15(2H, s), 4.19(1H, m), 5.33–5.48 (2H,m), 5.97(1H, d, J=8.7 Hz), 6.56(1H, d, J=3.9 Hz), 7.03–7.13 (3H, m),7.26(1H, d, J=3.9 Hz). IR(CHCl₃): 3518, 3450, 3431, 2671, 1739, 1709,1641, 1543, 1506, 1471 cm⁻¹. [α]_(D) ²⁴+43.7±0.8°(c=1.004, MeOH) Anal.(C₃₀H₃₉FNO₃S.0.1H₂O) Calcd.(%): C, 72.72; H, 7.97; N, 2.83; S, 6.47.Found(%): C, 72.68; H, 7.95; N, 2.96; S, 6.48.

Compound Number II-195

¹H-NMR(CDCl₃) δ: 0.94(1H, d, J=9.9 Hz), 1.09 and 1.21(each 3H, each s),1.53–2.50(14H, m), 4.19(1H, m), 4.32(2H, s), 5.34–5.47(2H, m), 6.00(1H,d, J=8.7 Hz), 6.76(1H, d, J=3.6 Hz), 7.28–7.39(3H, m), 7.50 (1H, m),7.66(1H, d, J=3.6 Hz). IR(CHCl₃): 3516, 3450, 3431, 2669, 1741, 1709,1643, 1543, 1508, 1456, 1315, 1163, 1126, 1059, 1038 cm⁻¹. [α]_(D)²⁵+36.4±0.7°(c=1.03, CHCl₃) Anal. (C₂₉H₃₄F₃NO₃S) Calcd.(%): C, 65.27; H,6.42; N, 2.62; S, 6.01. Found(%): C, 65.34; H, 6.30; N, 2.82; S, 6.00.

Compound Number II-197

¹H-NMR(CDCl₃) δ: 0.93(1H, d, J=10.5 Hz), 1.08 and 1.20(each 3H, eachs),1.49–2.42(14H, m), 3.22(2H, t, J=8.7 Hz), 4.07(2H, s), 4.20 (1H, m),4.57(2H, t, J=8.7 Hz), 5.33–5.48(2H, m), 5.99(1H, d, J=9.0 Hz), 6.79(1H, t, 7.5 Hz), 6.80(1H, d, J=3.6 Hz), 6.95(1H, d, J=7.5 Hz), 7.09(1H,d, J=7.5 Hz), 7.30(1H, d, J=3.6 Hz). IR(CDCl₃): 3514, 3450, 3431, 2667,1739, 1709, 1641, 1545, 1506, 1458 cm⁻¹. [α]_(D) ²⁵+42.0±0.8°(c=1.004,MeOH), Anal. (C₃₀H₃₇NO₄S.0.1H₂O) Calcd.(%): C, 70.72; H, 7.36; N, 2.75;S, 6.29. Found(%): C, 70.59; H, 7.39; N, 2.95; S, 6.31.

Compound Number II-198

¹H-NMR(CDCl₃) δ: 0.92 (1H, d, J=10.5 Hz), 1.07 and 1.19 (each 3H, eachs),1.47–2.41(14H, m), 4.20(1H, m), 4.24(2H, s), 5.32–5.47(2H, m),6.00(1H, d, J=8.7 Hz), 6.78(1H, d, J=3.9 Hz), 7.21(1H, dd, J=1.8 and 8.4Hz), 7.26(1H, d, J=5.7 Hz), 7.33(1H, d, J=3.9 Hz), 7.43(1H, d, J=5.7Hz), 7.67(1H, d, J=1.8 Hz), 7.81(1H, d, J=8.4 Hz). IR(CHCl₃): 3516,3450, 3431, 1739, 1709, 1641, 1545, 1458 cm⁻¹. [α]_(D)²⁵+40.9±0.8°(c=1.002, MeOH), Anal. (C₃₀H₃₅NO₃S₂.0.3H₂O) Calcd.(%): C,68.36; H, 6.81; N, 2.66; S, 12.17. Found(%): C, 68.30; H, 6.68; N, 2.94;S, 12.25.

Compound Number II-199

¹H-NMR(CDCl₃) δ: 0.93(1H, d, J=10.5 Hz), 1.07 and 1.20(each 3H, eachs),1.49–2.42(14H, m), 4.20(1H, m), 4.27(2H, s), 5.32–5.48(2H, m),5.99(1H, d, J=8.7 Hz), 6.80(1H, d, J=3.6 Hz), 7.24(1H, dd, J=1.5 and 8.1Hz), 7.31(1H, dd, J=0.6 and 5.4 Hz), 7.33(1H, d, J=3.6 Hz), 7.40 (1H, d,J=5.4 Hz), 7.73(1H, m), 7.77(1H, d, J=8.1 Hz). IR (CHCl₃): 3516, 3450,3431, 1741, 1709, 1641, 1543, 1508, 1469 cm⁻¹. [α]_(D)²⁵+41.5±0.8°(c=1.002, MeOH), Anal. (C₃₀H₃₅NO₃S₂.0.3H₂O) Calcd.(%): C,68.36; H, 6.81; N, 2.66; S, 12.17. Found(%): C, 68.37; H, 6.73; N, 2.86;S, 12.21.

Compound Number II-200

¹H-NMR(CDCl₃) δ: 0.93(1H, d, J=10.2 Hz), 1.06 and 1.19(each 3H, eachs),1.48–2.41(14H, m), 4.19(1H, m), 4.39(2H, s), 5.32–5.47(2H, m),5.99(1H, d, J=8.7 Hz), 6.86(1H, d, J=3.6 Hz), 7.21(1H, d, J=7.2 Hz),7.30(1H, d, J=3.6 Hz), 7.35(1H, t, J=7.2 Hz), 7.36(1H, d, J=5.4 Hz),7.42(1H, d, J=5.4 Hz), 7.74(1H, d, J=7.2 Hlz). IR(CHCl₃): 3516, 3450,3431, 1739, 1709, 1641, 1543, 1508, 1471, 1460 cm⁻¹. [α]_(D)²⁵+42.0±0.8°(c=1.001, MeOH), Anal. (C₃₀H₃₅NO₃S₂.0.3H₂O) Calcd.(%): C,68.36; H, 6.81; N, 2.66; S, 12.17. Found(%): C, 68.63; H, 6.78; N, 2.84;S, 12.26.

Compound Number II-201

¹H-NMR(CDCl₃) δ: 0.92(1H, d, J=10.2 Hz), 1.07 and 1.20(each 3H, eachs),1.52–2.47(14H, m), 4.20(1H, m), 4.23(2H, s), 5.32–5.51(2H, m),6.08(1H, d, J=8.7 Hz), 6.75(1H, d, J=3.6 Hz), 6.95(1H, dd, J=2.4 and 9.0Hz), 7.10(1H, d, J=2.4 Hz), 7.19(1H, s), 7.27(1H, d, J=3.6 Hz), 7.66(1H,d, J=9.0 Hz). IR(CHCl₃): 3427, 3249, 1707, 1633, 1601, 1545, 1510, 1442cm⁻¹. [α]_(D) ²⁵+40.1±0.8°(c=1.007, MeOH), Anal. (C₃₀H₃₅NO₄S₂.0.3H₂O)Calcd.(%): C, 66.34; H, 6.61; N, 2.58; S, 11.81. Found(%): C, 66.21; H,6.70; N, 2.70; S, 11.75.

Compound Number II-202

¹H-NMR(CDCl) δ: 0.93(1H, d, J=10.2 Hz), 1.08 and 1.21(each 3H, each s),1.53–2.45(14H, m), 4.17(1H, m), 4.24(2H, m), 4.69(2H, m), 5.35–5.47(2H,m), 6.02(1H, d, J=9.3 Hz), 6.72(1H, d, J=3.9 Hz), 7.23–7.31(4H, m),7.40(1H, m). IR(CHCl₃): 3516, 3450, 3431, 1709, 1641, 1527, 1508, 1456cm⁻¹. [α]_(D) ²⁶+32.7±0.7°(c=1.00, CHCl₃)

Compound Number II-203

¹H-NMR(CDCl₃) δ: 0.92(1H, d, J=10.2 Hz), 1.08 and 1.21(each 31H, eachs), 1.54–2.48(18H, m), 3.20 (4H, m), 4.11–4.22(3H, m), 4.43(2H, s),5.33–5.55(2H, m), 5.99(1H, d, J=8.4 Hz), 6.67(1H, d, J=4.2 Hz),7.30–7.43 (4H, m), 7.64(1H, d, J=4.2 Hz). IR(CHCl₃): 3514, 3448, 3420,2555, 2459, 1711, 1643, 1543, 1508, 1456 cm⁻¹. [α]_(D)²⁶+20.4±0.6°(c=1.05, CHCl₃) Anal. (C₃₃H₄₄N₂O₃S.1.1H₂O) Calcd.(%): C,69.71; H, 8.19; N, 4.93; S, 5.64. Found(%): C, 69.69; H, 8.08; N, 4.92;S, 5.54.

Compound Number II-204

¹H-NMR(CDCl₃) δ: 0.93(1H, d, J=10.5 Hz), 1.07 and 1.21(each 3H, each s),1.53–2.46(14H, m), 2.49(6H,s), 3.79(1H, d, J=10.8 Hz), 3.84 (1H, d,J=10.8 Hz), 4.19(1H, m), 4.35(1H, d, J=20.1 Hz), 4.37(1H, d, J=20.1 Hz),5.36–5.54 (2H, m), 5.94(1H, d, J=9.0 Hz), 6.71(1H, d, J=3.6 Hz),7.25–7.43(5H, m). IR(CHCl₃): 3516, 3448, 3429, 2553, 2459, 1711, 1643,1545, 1506, 1471 cm⁻¹. [α]_(D) ²⁶+20.9±0.6°(c=1.03, CHCl₃) Anal.(C₃₁H₄₂N₂O₃S.3.1H₂O) Calcd.(%): C, 64.35; H, 8.40; N, 4.84; S, 5.54.Found(%): C, 64.36; H, 7.87; N, 4.63; S, 5.17.

Compound Number II-205

¹H-NMR(CDCl₃) δ: 0.98(1H, d, J=10.5 Hz), 1.13 and 1.24(each 3H, each s),1.53–2.47(14H, m), 3.20–3.27(4H, m), 4.28(1H, m), 5.35–5.51 (2H, m),6.32(1H, d, J=8.4 Hz), 7.24(1H, d, J=7.5 Hz), 7.34 and 7.46 (each 1H,each m), 7.55(1H, dd, J=1.8 and 8.4 Hz), 7.67(1H, d, J=1.8 Hz),8.00–8.04(2H, m). IR(CHCl₃): 3518, 3448, 1709, 1649, 1597, 1514, 1294cm⁻¹. [α]_(D) ²⁵+58.8±1.0°(c=1.001, MeOH) Anal. (C₃₂H₃₇NO₄.0.2H₂O)Calcd.(%): C, 76.37; H, 7.49; N, 2.78. Found(%): C, 76.33; H, 7.50; N,2.88.

Compound Number II-206

¹H-NMR(CDCl₃) δ: 0.95(1H, d, J=10.2 Hz), 1.07 and 1.22(each 3H, each s),1.51–2.43(14H, m), 3.97(2H, s), 4.21(1H, m), 5.34–5.49(2H, m), 6.07(1H,d, J=3.3 Hz), 6.38(1H, d, J=9.3 Hz), 6.98–7.04(3H, m), 7.13–7.22(2H, m).IR (CHCl₃): 3518, 3438, 1739, 1709, 1651, 1606, 1549, 1508 cm⁻¹. [α]_(D)²⁶+57.2±1.0°(c=1.016, MeOH) Anal. (C₂₈H₃₄FNO₄.0.1H₂O) Calcd.(%): C,71.65; H, 7.34; N, 2.98; F, 4.05. Found(%): C, 71.57; H, 7.44; N, 3.14;F, 4.01.

Compound Number II-207

¹H-NMR(CDCl₃) δ: 0.96(1H, d, J=10.5 Hz), 1.07 and 1.21(each 3H, each s),1.52–2.43(14H, m), 4.00(2H, s), 4.21(1H, m), 5.34–5.49(2H, m), 6.09(1H,d, J=3.3 Hz), 6.40(1H, d, J=9.6 Hz), 7.01(1H, d, J=3.3 Hz),7.22–7.36(5H, m). IR (CHCl₃): 3516, 3439, 2667, 1738, 1709, 1651, 1606,1547, 1498 cm⁻¹. [α]_(D) ²⁴+62.2±1.0°(c=1.007, MeOH) Anal.(C₂₈H₃₅NO₄.0.2H₂O) Calcd.(%): C, 74.21; H, 7.87; N, 3.09. Found(%): C,74.14; H, 7.81; N, 3.25.

Compound Number II-208

¹H-NMR(CDCl₃) δ: 0.92(1H, d, J=10.2 Hz), 1.07 and 1.20(each 3H, eachs),1.48–2.42(14H, m), 4.19(1H, m), 4.42(2H, s), 5.32–5.47(2H, m),5.98(1H, d, J=8.7 Hz), 6.78(1H, d, J=2.1 Hz), 6.84(1H, d, J=3.9 Hz),7.13(1H, dd, J=1.5 and 7.5 Hz), 7.19(1H, t, J=7.5 Hz), 7.30(1H, d, J=3.9Hz), 7.50(1H, dd, J=1.5 and 7.5 Hz), 7.63(1H, d, 2.1 Hz). IR(CHCl₃):3516, 3450, 3431, 1741, 1709, 1641, 1543, 1508, 1471, 1458, 1427 cm⁻¹.[α]_(D) ²⁵+43.5±0.8°(c=1.010, MeOH), Anal. (C₃₀H₃₅NO₄S.0.2H₂O)Calcd.(%): C, 70.75; H, 7.01; N, 2.75; S, 6.30. Found(%): C, 70.80; H,7.02; N, 2.96; S, 6.26.

Compound Number II-209

¹H-NMR(CDCl₃) δ: 0.94(1H, d, J=10.2 Hz), 1.09 and 1.22(each 3H, each s),1.55–2.41(14H, m), 2.95(3H, s), 4.18–4.21(3H, m), 4.45(2H, s),5.39–5.43(2H, m), 6.00(1H, d, J=8.7 Hz), 6.63–6.71(4H, m), 7.16–7.26(6H,m), 7.32(1H, m). IR(CHCl₃): 3516, 3450, 3431, 1739, 1709, 1643, 1599,1543, 1505, 1454 cm⁻¹. [α]_(D) ²⁶+32.2±0.7°(c=1.00, CHCl₃) Anal.(C₃₆H₄₄N₂O₃S.0.6H₂O) Calcd.(%): C, 72.59; H, 7.65; N, 4.70; S, 5.38.Found(%): C, 72.68; H, 7.47; N, 4.74; S, 5.29.

Compound Number II-211

¹H-NMR(CDCl₃) δ: 0.93(1H, d, J=9.9 Hz), 1.07 and 1.20(each 3H, each s),1.49–2.41(14H, m), 4.19(1H, m), 4.30(2H, s), 5.32–5.48(2H, m), 5.99(1H,d, J=9.0 Hz), 6.82(1H, d, J=3.6 Hz), 7.24(1H, dd, J=1.5 and 8.1 Hz),7.30–7.36(2H, m), 7.4–7.47(2H, m), 7.55(1H, d, J=8.1 Hz), 7.87–7.94(2H,m). IR(CHCl₃): 3510, 3450, 3431, 2669, 1739, 1709, 1641, 1545, 1506,1458, 1429 cm⁻¹. [α]_(D) ²⁴+39.4±0.8°(c=1.002, MeOH) Anal.(C₃₄H₃₇NO₄S.0.1H₂O) Calcd.(%): C, 73.25; H, 6.73; N, 2.51; S, 5.75.Found(%): C, 73.13; H, 6.53; N, 2.69; S, 5.79.

Compound Number II-212

¹H-NMR(CDCl₃) δ: 0.93(1H, d, J=10.2 Hz), 1.08 and 1.21(each 3H, each s),1.50–2.43(14H, m), 3.79 and 3.86(each 3H, each s), 4.14(2H, s), 4.19(1H,m), 5.33–5.48(2H, m), 5.96(1H, d, J=8.4 Hz), 6.78–6.85 (3H, m), 7.00(1H,t, J=8.1 Hz), 7.30(1H, d, J=3.6 Hz). IR(CHCl₃): 3516, 3450, 3431, 2667,1739, 1709, 1641, 1543, 1506, 1481, 1273, 1076 cm⁻¹. [α]_(D)²⁶+39.6±0.8°(c=1.007, MeOH) Anal. (C₃₀H₃₉NO₅S.0.1H₂O) Calcd.(%): C,68.31; H, 7.49; N, 2.66; S, 6.08. Found(%): C, 68.17; H, 7.50; N, 2.76;S, 6.13.

Compound Number II-213

¹H-NMR(CDCl₃) δ: 0.94(1H, d, J=10.2 Hz), 1.09 and 1.22 (each 3H, eachs),1.51–2.45(14H, m), 2.39(3H, s), 4.15(2H, s), 4.21(1H, m), 5.34–5.50(2H, m), 5.87(1H, s), 6.04(1H, d, J=8.7 Hz), 6.86(1H, d, J=3.6 Hz),7.32(1H, d, J=3.6 Hz). IR(CHCl₃): 3514, 3450, 3431, 1709, 1645, 1608,1545, 1508, 1471, 1456 cm⁻¹. [α]_(D) ²⁵+47.0±0.9°(c=1.017, MeOH), Anal.(C₂₆H₃₄N₂O₄S.0.3H₂O) Calcd.(%): C, 65.60; H, 7.33; N, 5.88; S, 6.74.Found(%): C, 65.49; H, 7.31; N, 6.00; S, 6.86.

Compound Number II-214

¹H-NMR(CDCl₃) δ: 0.93(1H, d, J=10.2 Hz), 1.08 and 1.21(each 3H, eachs),1.50–2.42(14H, m), 2.33(3H, s), 3.82(3H, s), 4.07(2H, s), 4.18 (1H,m), 5.33–5.48(2H, m), 5.96(1H, d, J=8.7 Hz), 6.69(1H, s), 6.74 (1H, d,J=7.8 Hz), 6.76(1H, d, J=3.6 Hz), 7.03(1H, d, J=7.8 Hz), 7.28 (1H, d,J=3.6 Hz). IR(CHCl₃): 3516, 3450, 3431, 1741, 1709, 1639, 1614, 1543,1506, 1464 cm⁻¹. [α]_(D) ²⁴+43.3±0.8°(c=1.012, MeOH), Anal.(C₃₀H₃₉NO₄S.0.1H₂O) Calcd.(%): C, 70.45; H, 7.73; N, 2.74; S, 6.27.Found(%): C, 70.35; H, 7.78; N, 2.96; S, 6.20.

Compound Number II-215

¹H-NMR(CDCl₃) δ: 0.93(1H, d, J=10.2 Hz), 1.07 and 1.21(each 3H, eachs),1.49–2.43(14H, m), 3.84(3H, s), 4.20(1H, m), 4.32(2H, s),5.33–5.48(2H, m), 5.99(1H, d, J=8.4 Hz), 6.83(1H, d, J=3.6 Hz), 7.01(1:H, dd, J=2.4 and 8.7 Hz), 7.12(1H, d,J=2.4 Hz), 7.21(1H, s), 7.31(1H, d, J=3.6 Hz), 7.71(1H, d, J=8.7 Hz). IR(CDCl₃): 3516, 3450, 3431,1739, 1709, 1643, 1601, 1543, 1508, 1458, 1427 cm⁻¹. [α]_(D)²⁵+38.5±0.8°(c=1.004, MeOH), Anal. (C₃₁H₃₇NO₄S₂.0.1H₂O) Calcd.(%): C,67.26; H, 6.72; N, 2.53; S, 11.58. Found(%): C, 67.24; H, 6.73; N, 2.77;S, 11.51.

Compound Number II-216

¹H-NMR(CDCl₃) δ: 0.94(1H, d, J=10.5 Hz), 1.07 and 1.20(each 3H, each s),1.50–2.42(14H, m), 3.87(2H, s), 4.18(1H, m), 4.20(2H, s), 5.32–5.48 (2H,m), 5.98(1H, d, J=7.2 Hz), 6.81(1H, d, J=3.6 Hz), 7.23–7.41 (5H, m),7.53(1H, d, J=7.5 Hz), 7.71–7.77(2H, m). IR(CHCl₃): 3514, 3450, 3431,1739, 1709, 1641, 1545, 1506, 1469, 1456 cm⁻¹. [α]_(D)²⁵+38.5±0.8°(c=1.007, MeOH) Anal. (C₃₅H₃₉NO₃S.0.2H₂O) Calcd.(%): C,75.42; H, 7.13; N, 2.51; S, 5.75. Found(%): C, 75.36; H, 7.18; N, 2.79;S, 5.50.

Compound Number II-217

¹H-NMR(CDCl₃) δ: 0.96(1H, d, J=10.2 Hz), 1.10 and 1.21(each 3H, each s),1.52–2.44(14H, m), 3.14–3.24(4H, m), 4.13(2H, s), 4.24(1H, m),5.32–5.49(2H, m), 6.19(1H, d, J=9.0 Hz), 7.06–7.18(4H, m), 7.22 (1H, d,J=8.1 H), 7.39(1H, dd, J=1.8 and 8.1 Hz), 7.51(1H, d, J=1.8 Hz).IR(CHCl₃): 3516, 3452, 1738, 1709, 1649, 1570, 1518, 1491, 1471 cm⁻¹.[α]_(D) ²⁵+54.4±0.9°(c=1.002, MeOH) Anal. (C₃₂H₃₉NO₄.0.1H₂O) Calcd.(%):C, 78.85; H, 8.11.; N, 2.87. Found(%): C, 78.74; H, 8.14; N, 3.17.

Compound Number II-218

¹H-NMR(CDCl₃) δ: 0.94(1H, d, J=10.2 Hz), 1.08 and 1.21(each 3H, each s),1.50–2.43(14H, m), 3.83, 3.85 and 3.86(each 3H, each s), 4.07 (2H, s),4.19(1H, m), 5.33–5.49(2H, m), 5.97(1H, d, J=9.0 Hz), 6.62 (1H, d, J=8.7Hz), 6.76(1H, td, J=0.9 and 3.6 Hz), 6.87(1H, d, J=8.7 Hz), 7.30 (1H, d,(1, J=3.6 Hz). IR(CHCl₃): 3516, 3450, 3431, 1739, 1709, 1641, 1603,1543, 1495, 1469, 1277, 1259, 1097 cm⁻¹. [α]_(D) ²⁶+38.4±0.8°(c=1.013,MeOH) Anal. (C₃₁H₄₁NO₆S.0.2H₂O) Calcd.(%): C, 66.57; H, 7.46; N, 2.50;S, 5.73. Found(%): C, 66.54; H, 7.42; N, 2.61; S, 5.71.

Compound Number II-219

¹H-NMR(CDCl₃) δ: 0.94(1H, d, J=10.2 Hz), 1.08 and 1.21(each 3H, each s),1.50–2.42(14H, m), 2.18 and 2.29(each 3H, each s), 4.14(2H, s), 4.19(1H,m), 5.33–5.49(2H, m), 5.96(1H, d, J=8.4 Hz), 6.67(1H, td, J=0.9 and 3.6Hz), 7.02–7.12(3H, m), 7.29(1H, t, J=3.6 Hz). IR (CDCl₃): 3516, 3450,3431, 1741, 1709, 1641, 1543, 1506, 1471 cm⁻¹. [α]_(D)²⁶+42.8±0.8°(c=1.007, MeOH) Anal. (C₃₀H₃₉NO₃S) Calcd.(%): C, 72.98; H,7.96; N, 2.84; S, 6.50. Found(%): C, 72.67; H, 7.98; N, 2.94; S, 6.38.

Compound Number II-220

¹H-NMR(CDCl₃) δ: 0.95(1H, d, J=10.2 Hz), 1.09 and 1.22(each 3H, each s),1.51–2.44(14H, m), 3.83(3H, s), 3.84(6H, s), 4.07(2H, s), 4.20 (1H, m),5.34–5.49(2H, m), 6.00(1H, d, J=8.7 Hz), 6.45(2H, s), 6.79 and 7.31(each 1H, each d, each J=3.6 Hz). IR(CHCl₃): 3516, 3450, 3431, 1741,1709, 1641, 1593, 1543, 1506, 1464, 1421, 1331, 1240, 1130 cm⁻¹. [α]_(D)²⁴+38.3±0.8°(c=1.004, MeOH) Anal. (C₃₁H₄₁NO₆S.0.2H₂O) Calcd.(%): C,66.57; H, 7.46; N, 2.50; S, 5.73. Found(%): C, 66.48; H, 7.37; N, 2.59;S, 5.63.

Compound Number II-221

¹H-NMR(CDCl₃) δ: 0.94(1H, d, J=10.2 Hz), 1.08 and 1.21(each 3H, each s),1.50–2.43(14H, m), 4.08(2H, s), 4.20(1H, m), 5.33–5.49(2H, m), 5.95(2H,s), 5.99(1H, d, J=8.7 Hz), 6.68–6.82(4H, m), 7.30(1H, d, J=3.6 Hz).IR(CHCl₃): 3512, 3450, 3431, 1739, 1709, 1641, 1545, 1506, 1460, 1252,1063 cm⁻¹. [α]_(D) ²⁴+41.8±0.8°(c=1.007, MeOH) Anal. (C₂₉H₃₅NO₅S)Calcd.(%): C, 68.34; H, 6.92; N, 2.75; S, 6.29. Found(%): C, 68.04; H,6.90; N, 2.79; S, 6.29.

Compound Number II-222

¹H-NMR(CDCl₃) δ: 0.92(1H, d, J=10.5 Hz), 1.09 and 1.21(each 3H, each s),1.51–2.45(14H, m), 2.14(3H, s), 4.08(2H, s), 4.18(1H, m), 5.32–5.50 (2H,m), 6.08(1H, d, J=8.4 Hz), 6.76(1H, d, J=3.6 Hz), 6.97 (1H, d, J=7.8Hz), 7.24(1H, t, J=8.4 Hz), 7.30(1H, d, J=3.6 Hz), 7.38–7.40 (2H, m),7.74(1H, br s). IR(CHCl₃): 3514, 3435, 3311, 1705, 1639, 1612, 1534,1508, 1439 cm⁻¹. [α]_(D) ²⁵+40.1±0.8°(c=1.008, MeOH) Anal.(C₃₀H₃₈N₂O₄S.0.4H₂O) Calcd.(%): C, 68.00; H, 7.38; N, 5.29; S, 6.05.Found(%): C, 68.11; H, 7.17; N, 5.22; S, 5.93.

Compound Number II-223

¹H-NMR(CDCl₃) δ: 0.94(1H, d, J=10.5 Hz), 1.09 and 1.22(each 3H, each s),1.53–2.50(14H, m), 2.99(3H, s), 4.13(2H, s), 4.21(1H, m), 5.34–5.52 (2H,m), 6.02(1H, d, J=9.3 Hz), 6.80(1H, d, J=3.9 Hz), 7.04–7.07(2H, m),7.16(1H, m), 7.25–7.32(3H, m). IR(CHCl₃): 3510, 3440, 3431, 3371, 1709,1639, 1608, 1543, 1508, 1471, 1386, 1335, 1151 cm⁻¹. [α]_(D)²⁴+38.3±0.8°(c=1.006, MeOH) Anal. (C₂₉H₃₈N₂O₅S₂.0.2H₂O) Calcd.(%): C,61.94; H, 6.88; N, 4.98; S, 11.40. Found(%): C, 61.99; H, 6.92; N, 4.95;S, 10.97.

Compound Number II-224

¹H-NMR(CDCl₃) δ: 0.94(1H, d, J=10.2 Hz), 1.09 and 1.21(each 3H, each s),1.50–2.44(14H, m), 4.21(1H, m), 4.32(2H, s), 5.34–5.50(2H, m), 6.01(1H,d, J=9.0 Hz), 6.86, 6.88 and 7.14(each 1H, each d, each J=3.6 Hz),7.23–7.37(4H, m), 7.53–7.56(2H, m).

Compound Number II-225

¹H-NMR(CDCl₃) δ: 0.94 (1H, d, J=10.2 Hz), 1.08 and 1.21(each 311, eachs), 1.50–2.43(14H, m), 4.08(2H, s), 4.17–4.30(5H, m), 5.33–5.49 (2H, m),5.98(1H, d, J=8.4 Hz), 6.71–6.80(4H, m), 7.28(1H, d, J=3.6 Hz).IR(CHCl₃): 3516, 3450, 3431, 1739, 1709, 1639, 1602, 1543, 1506, 1475,1456, 1284, 1090 cm⁻¹. [α]_(D) ^(24.5)+40.2±0.8°(c=1.011, MeOH) Anal.(C₃₀H₃₇NO₅S.0.2H₂O) Calcd.(%): C, 68.34; H, 7.15; N, 2.66; S, 6.08.Found(%): C, 68.35; H, 7.03; N, 2.71; S, 6.17.

Compound Number II-226

¹H-NMR(CDCl₃) δ: 0.94(1H, d, J=10.2 Hz), 1.08 and 1.21(each 3H, each s),1.50–2.43(14H, m), 2.31 and 3.70(each 3H, each s), 4.15(2H, s), 4.19(1H,m), 5.33–5.49(2H, m), 5.98(1H, d, J=8.7 Hz), 6.77(1H, d, J=3.9 Hz),6.96–7.11(3H, m), 7.31(1H, d, J=3.9 Hz). IR(CHCl₃): 3516, 3450, 3431,2669, 1738, 1709, 1641, 1545, 1506, 1471, 1259, 1011 cm⁻¹. [α]_(D)²⁴+41.2±0.8°(c=1.003, MeOH) Anal. (C₃₀H₃₉NO₄S) Calcd.(%): C, 70.69; H,7.71; N, 2.75; S, 6.29. Found(%): C, 70.41; H, 7.76; N, 2.97; S, 6.04.

Compound Number II-227

¹H-NMR(CDCl₃) δ: 0.93(1H, d, J=10.2 Hz), 1.08 and 1.21(each 3H, each s),1.51–2.42(14H, m), 2.16(3H, s), 4.09(2H, s), 4.18(1H, m), 5.32–5.50 (2H,m), 6.01(1H, d, J=8.7 Hz), 6.77(1H, d, J=3.6 Hz), 7.17 (2H, d, J=8.1Hz), 7.32(1H, d, J=3.6 Hz), 7.43(1H, br s), 7.44(2H, d, J=8.1 Hz).IR(CHCl₃): 3514, 3435, 3311, 1705, 1639, 1541, 1513, 1410 cm⁻¹. [α]_(D)^(24.5)+40.8±0.8°(c=1.000, MeOH) Anal. (C₃₀H₃₈N₂O₄S.0.4H₂O) Calcd.(%):C, 68.00; H, 7.38; N, 5.29; S, 6.05. Found(%): C, 68.06; H, 7.38; N,5.28; S, 5.92.

Compound Number II-228

¹H-NMR(CDCl₃) δ: 0.94(1H, d, J=9.9 Hz), 1.09 and 1.21(each 3H, each s),1.51–2.42(14H, m), 2.99(3H, s), 4.11(2H, s), 4.20(1H, m), 5.33–5.49(2H,m), 6.01(1H, d, J=9.3 Hz), 6.78(1H, d, J=3.6 Hz), 6.86 (1H, br s),7.17–7.25(4H, m), 7.31(1H, d, J=3.6 Hz). IR(CHCl₃): 3510, 3448, 3431,3371, 1707, 1639, 1543, 1510, 1471, 1456, 1387, 1330, 1155 cm⁻¹. [α]_(D)^(24.5)+37.6±0.8°(c=1.006, MeOH) Anal. (C₂₉H₃₈N₂O₅S₂.0.3H₂O) Calcd.(%):C, 61.74; H, 6.90; N, 4.97; S, 11.37. Found(%): C, 61.84; H, 6.93; N,5.03; S, 11.14.

Compound Number II-229

mp.149–150° C. ¹H-NMR(CDCl₃) δ: 0.92(1H, d, J=10.5 Hz), 1.05 and1.19(each 3H, each s), 1.47–2.40(14H, m), 4.18(1H, m), 4.40 (2H, s),5.31–5.46(2H, m), 5.98(1H, d, J=8.4 Hz), 6.88(1H, d, J=3.9 Hz),7.30–7.35(2H, m), 7.42–7.48(3H, m), 7.58(1H, m), 8.08(1H, d, J=6.6 Hz),8.14(1H, m). IR(CHCl₃): 3514, 3450, 3431, 2667, 1738, 1707, 1643, 1543,1508, 1471, 1458, 1444 cm⁻¹. [α]_(D) ^(24.5)+39.7±0.8°(c=1.008, MeOH)Anal. (C₃₄H₃₇NO₃S₂) Calcd.(%): C, 71.42; H, 6.52; N, 2.45; S, 11.22.Found(%): C, 71.21; H, 6.53; N, 2.51; S, 10.97.

Compound Number II-230

¹H-NMR(CDCl₃) δ: 0.92(1H, d, J=10.5 Hz), 1.06 and 1.19(each 3H, each s),1.48–2.40(14H, m), 3.79(2H, s), 4.18(1H, m), 4.26(2H, s), 5.21–5.47(2H,m), 5.96(1H, d, J=8.4 Hz), 6.78(1H, d, J=3.6 Hz), 7.18 (1H, d, J=7.2Hz), 7.27–7.40(4H, m), 7.53(1H, d, J=7.2 Hz), 7.72(1H, d, J=7.8 Hz),7.78(1H, d, J=6.9 Hz). IR(CHCl₃): 3510, 3450, 3431, 2669, 1739, 1709,1641, 1543, 1506, 1471, 1456 cm⁻¹. [α]_(D) ²⁴+36.6±0.8°(c=1.006, MeOH)Anal. (C₃₅H₃₉NO₃S.0.2H₂O) Calcd.(%): C, 75.42; H, 7.13; N, 2.51; S,5.75. Found(%): C, 75.46; H, 7.15; N, 2.73; S, 5.55.

Compound Number II-231

¹H-NMR(CDCl₃) δ: 0.93(1H, d, J=9.9 Hz), 1.08 and 1.21(each 3H, each s),1.50–2.43(14H, m), 2.20, 2.45 and 3.67(each 3H, each s), 4.13 (2H, s),4.19(1H, m), 5.33–5.49(2H, m), 5.97(1H, d, J=8.4 Hz), 6.77 (1H, td,J=0.9 and 3.9 Hz), 6.89 and 6.95(each 1H, each d, each J=7.8 Hz),7.31(1H, d, J=3.6 Hz). IR(CHCl₃): 3516, 3450, 3431, 1738, 1709, 1641,1545, 1506, 1458, 1263, 1084, 1009 cm⁻¹. [α]_(D) ²⁴+39.8±0.8°(c=1.006,MeOH) Anal. (C₃₁H₄₁NO₄S) Calcd.(%): C, 71.09; H, 7.89; N, 2.67; S, 6.12.Found(%): C, 70.80; H, 8.02; N, 2.92; S, 6.06.

Compound Number II-232

¹H-NMR(CDCl₃) δ: 0.93(1H, d, J=10.2 Hz), 1.06 and 1.19(each 3H, each s),1.49–2.41(14H, m), 4.18(1H, m), 4.50(2H, s), 5.32–5.47(2H, m), 5.98(1H,d, J=9.0 Hz), 6.89(1H, d, J=3.9 Hz), 7.29–7.38(4H, m), 7.47 (1H, m),7.59(1H, d, J=8.4 Hz), 7.86(1H, m), 7.95(1H, d, J=7.8 Hz). IR(CHCl₃):3510, 3450, 3431, 2669, 1739, 1709, 1641, 1545, 1508, 1471, 1450, 1423cm⁻¹. [α]_(D) ²⁴+40.3±0.8°(c=1.007, MeOH) Anal. (C₃₄H₃₇NO₄S.0.2H₂O)Calcd.(%): C, 73.01; H, 6.74; N, 2.50; S, 5.73. Found(%): C, 72.91; 11,6.58; N, 2.59; S, 5.75.

Compound Number II-233

¹H-NMR(CDCl₃) δ: 0.92(1H, d, J=10.2 Hz), 1.08 and 1 .20(each 3H, eachs),1.50–2.43(14H, m), 4.04(2H, s), 4.20(1H, m), 5.32–5.49(2H, m),6.03(1H, d, J=9.0 Hz), 6.75(1H, d, J=3.6 Hz), 6.80 and 7.06(each 2H,each d, J=8.7 Hz), 7.32(1H, d, J=3.6 Hz). IR(CHCl₃): 3446, 3510, 3182,2673, 1709, 1635, 1614, 1545, 1512, 1471, 1458 cm⁻¹. [α]_(D)²⁵+43.8±0.8°(c=1.000, MeOH), Anal. (C₂₈H₃₅NO₄S) Calcd.(%): C, 69.82; H,7.32; N, 2.91; S, 6.66. Found(%): C, 69.57; H, 7.43; N, 3.00; S, 6.61.

Compound Number II-295

mp.156–157° C. ¹H-NMR(CDCl₃) δ: 1.00(1H, d, J=10.2 Hz), 1.17 and 1.25(each 3H, each s), 1.57–2.51(14H, m), 4.31(1H, m), 5.34–5.54(2H, m),6.37(1H, d, J=9.3 Hz), 7.33–7.47(3H, m), 7.61(1H, s), 7.64(1H, m),7.70–7.73 (2H, m), 7.87(1H, d, J=8.4 Hz), 8.15(1H, d, J=1.2 Hz). IR(CHCl₃); 3518, 3452, 1741, 1709, 1649, 1510 cm⁻¹. [α]_(D)²³+67.2±2.1°(c=0.503, MeOH) Anal. (C₃₁H₃₅NO₃S.0.1H₂O) Calcd.(%): C,73.95; H, 7.05; N, 2.78; S, 6.37. Found(%): C, 73.94; H, 7.08; N, 3.04;S, 6.53.

Compound Number II-296

mp.126–127° C. ¹H-NMR(CDCl₃) δ: 0.93(1H, d, J=10.2 Hz), 1.08 and1.20(each 3H, each s), 1.50–2.46(14H, m), 4.17(1H, m), 5.33–5.51(2H, m),6.04(1H, d, J=8.4 Hz), 6.51(1H, dd, J=1.5 and 3.3 Hz), 7.13(1H, dd,J=2.7 and 3.3 Hz), 7.22(1H, dd, J=7.8 and 9.0 Hz), 7.73(1H, dd, J=1.5and 2.1 Hz), 7.91–7.96(2H, m). IR(CHCl₃): 3513, 3449, 3144, 1733, 1709,1651, 1592, 1507, 1496, 1385, 1181 cm⁻¹. [α]_(D) ²⁴+36.2±0.8°(c=1.005,MeOH) Anal. (C₂₇H₃₃FN₂O₅S) Calcd.(%): C, 62.77; H, 6.44; N, 5.42; F,3.68; S, 6.21. Found(%): C, 62.71; H, 6.49; N, 5.39; F, 3.69; S, 6.21.

Compound Number II-297

mp.145–146° C. ¹H-NMR(CDCl₃) δ: 0.93(1H, d, J=10.2 Hz), 1.08 and1.20(each 3H, each s), 1.50–2.45(14H, m), 3.86(3H, s), 4.17(1H, m),5.33–5.51 (2H, m), 6.04(1H, d, J=8.4 Hz), 6.48(1H, dd, J=1.5 and 3.3Hz), 6.98 and 7.85(each 2H, each d, each J=9.0 Hz), 7.12(1H, dd, J=2.7and 3.3 Hz), 7.71(1H, dd, J=1.8 and 2.1 Hz). IR(CHCl₃): 3513, 3449,3413, 3143, 1733, 1709, 1649, 1596, 1576, 1499, 1379, 1266, 1189, 1167cm⁻¹. [α]_(D) ²⁴+34.5±0.7°(c=1.005, MeOH) Anal. (C₂₈H₃₆N₂O₆S) Calcd.(%):C, 63.61; H, 6.86; N, 5.30; S, 6.07. Found(%): C, 63.54; H, 6.93; N,5.18; S, 6.08.

Compound Number II-298

¹H-NMR(CDCl₃) δ: 0.97(1H, d, J=10.5 Hz), 1.12 and 1.23(each 3H, each s),1.50–2.50(14H, m), 4.23(1H, m), 5.39–5.51(2H, m), 6.09(1H, d, J=9.6 Hz),6.35(1H, dd, J=2.4 and 3.9 Hz), 6.48(1H, dd, J=2.4 and 3.9 Hz), 7.02(1H,dd, J=3.6 and 4.8 Hz), 7.18(1H, dd, J=0.6 and 4.8 Hz), 7.41(1H, dd,J=0.6 and 3.6 Hz), 10.92(1H, brs). IR(CHCl₃): 3506, 3447, 3220, 3164,1704, 1617, 1537, 1508 cm⁻¹. [α]_(D) ²⁴+50.7±0.9°(c=1.009, MeOH) Anal.(C₂₅H₃₂N₂O₃S.0.2H₂O) Calcd.(%): C, 67.59; H, 7.35; N, 6.31; S, 7.22.Found(%): C, 67.60; H, 7.23; N, 6.39; S, 7.34.

Compound Number II-299

¹H-NMR(CDCl₃) δ: 0.93(1H, d, J=10.2 Hz), 1.08 and 1.21(each 3H, each s),1.50–2.44(14H, m), 2.27(3H, s), 4.05(2H, s), 4.20(1H, m), 5.33–5.49(2H,m), 6.01(1H, d, J=8.7 Hz), 6.71(1H, d, J=3.9 Hz), 7.09 (1H, dd, J=1.2and 7.8 Hz), 7.17–7.32(3H, m), 7.28(1H, d, J=3.9 Hz). IR(CHCl₃): 3516,3450, 3431, 2669, 1747, 1709, 1641, 1543, 1506, 1456, 1369 cm⁻¹. [α]_(D)²⁴+40.2°±0.8°(c=1.006, MeOH) Anal. (C₃₀H₃₇NO₅S.0.2H₂O) Calcd.(%): C,68.34; H, 7.15; N, 2.66; S, 6.08. Found(%): C, 68.33; H, 6.94; N, 2.83;S, 6.31.

Compound Number II-300

¹H-NMR(CDCl₃) δ: 0.93(1H, d, J=9.9 Hz), 1.08 and 1.21(each 3H, each s),1.50–2.41(14H, m), 2.60(3H, s), 4.20(1H, m), 5.34–5.48(2H, m), 6.18(1H,d, J=8.7 Hz), 7.28(1H, d-like), 7.36(1H, d, J=3.9 Hz), 7.40 (1H,t-like), 7.51(1H, dt, J=1.2 and 7.2 Hz), 7.61(1H, d, J=3.9 Hz), 8.15(1H,dd, J=1.2 and 8.1 Hz). IR(CHCl₃): 3512, 3446, 1739, 1709, 1655, 1529,1504, 1325, 1157 cm⁻¹. [α]_(D) ²⁴+51.1±0.9°(c=1.010, MeOH) Anal.(C₂₈H₃₅NO₅S₂) Calcd.(%): C, 63.49; H, 6.66; N, 2.64; S, 12.11. Found(%):C, 63.23; H, 6.53; N, 2.70; S, 12.17.

Compound Number II-301

¹H-NMR(CDCl₃) δ: 0.93(1H, d, J=10.2 Hz), 1.07 and 1.21(each 3H, each s),1.50–2.40(14H, m), 2.42(3H, s), 4.20(1H, m), 5.34–5.47(2H, m), 6.17(1H,d, J=8.7 Hz), 7.32(1H, d-like), 7.34 and 7.57(each 1H, each d, eachJ=4.2 Hz), 7.86(2H, d-like). IR(CDCl₃): 3512, 3446, 1741, 1707, 1655,1529, 1504, 1331, 1153 cm⁻¹. [α]_(D) ²⁴+54.9±0.9°(c=1.008, MeOH) Anal.(C₂₈H₃₅NO₅S₂) Calcd.(%): C, 63.49; H, 6.66; N, 2.64; S, 12.11. Found(%):C, 63.16; H, 6.54; N, 2.70; S, 12.16.

Compound Number II-302

¹H-NMR(CDCl₃) δ: 0.96(1H, d, J=10.2 Hz), 1.14 and 1.25(each 3H, eachs),1.53–2.47(14H, m), 4.25(1H, m), 5.37–5.52(2H, m), 6.23(1H, d, J=8.7Hz), 7.16–7.22(2H, m), 7.36(1H, m), 7.46(1H, s), 7.45–7.49(1H, m).IR(CHCl₃): 3516, 3446, 3429, 1734, 1703, 1652, 1606, 1521, 1496, 1457,1419 cm⁻¹. [α]_(D) ²⁵+72.8°±1.1°(c=1.005, MeOH), Anal.(C₂₈H₃₁NO₄S.0.3H₂O) Calcd.(%): C, 69.63; H, 6.59; N, 2.90; S, 6.63.Found(%): C, 69.51; H, 6.72; N, 3.30; S, 6.56.

Compound Number III-1

¹H-NMR(CDCl₃) δ: 0.88(1H, d, J=10.2 Hz), 1.07 and 1.23(each 3H, each s),1.56–2.51(13H, m), 2.67(1H, m), 4.41(1H, m), 5.29–5.41(2H, m), 6.07(1H,d, J=8.1 Hz), 6.34 and 7.16(each 2H, each t, each J=2.1 Hz), 7.35 and7.52(each 1H, each d, each J=3.9 Hz). IR (CHCl₃): 3511, 3431, 3144,3101, 2668, 1708, 1656, 1530, 1505, 1455, 1384, 1167 cm⁻¹. [α]_(D)²⁴+34.2±0.7°(c=1.007, MeOH) Anal. (C₂₅H₃₂N₂O₅S₂.0.5H₂O) Calcd.(%): C,58.46; H, 6.48; N, 5.45; S, 12.48. Found(%): C, 58.77; H, 6.40; N, 5.65;S, 12.72.

Compound Number III-47

¹H-NMR(CDCl₃) δ: 0.94(1H, d, J=9.9 Hz), 1.07 and 1.23(each 3H, each s),1.56–2.48(13H, m), 2.68(1H, m), 4.42(1H, m), 5.29–5.42(2H, m), 6.16(1H,d, J=8.4 Hz), 7.16(1H, dd, J=3.9 and 5.1 Hz), 7.42 and 7.63(each 1H,each d, each J=3.9 Hz), 7.70(1H, dd, J=1.5 and 5.1 Hz), 7.76(1H, dd,J=1.5 and 3.9 Hz). IR (CHCl₃): 3516, 3431, 3365, 3097, 1708, 1654, 1530,1505, 1402, 1336, 1153 cm⁻¹. [α]_(D) ²⁴+34.5±0.7°(c=1.010, MeOH) Anal.(C₂₅H₃₁NO₅S₃.0.1H₂O) Calcd.(%): C, 57.36; H, 6.01; N, 2.68; S, 18.38.Found(%): C, 57.16; H, 5.88; N, 2.76; S, 18.36.

Compound Number III-55

¹H-NMR (CDCl₃) δ: 0.88(1H, d, J=9.9 Hz), 1.07 and 1.23(each 3H, each s),1.58–2.34(12H, m), 2.39(3H, s), 2.44(1H, m), 2.68(1H, m), 4.41(1H, m),5.29–5.42(2H, m), 5.99(1H, m), 6.08(1H, d, J=8.4 Hz), 6.20(1H, t, J=3.3Hz), 7.19(1H, m), 7.38 and 7.55(each 1H, each d, each J=3.9 Hz).IR(CHCl₃): 3510, 3431, 3150, 3100, 1708, 1656, 1530, 1505, 1375, 1161cm⁻¹. [α]_(D) ²⁴+30.9±0.7°(c=1.000, MeOH) Anal. (C₂₆H₃₄N₂O₅S₂.0.3H₂O)Calcd.(%): C, 59.58; H, 6.65; N, 5.35; 12.24. Found(%): C, 59.57; H,6.48; N, 5.51; S, 12.22.

Compound Number III-80

¹H-NMR(CDCl₃) δ: 0.90(1H, d, J=9.9 Hz), 1.06 and 1.23(each 3H, each s),1.58–2.48(13H, m), 2.67(1H, m), 4.41(1H, m), 5.29–5.42(2H, m), 6.27(1H,d, J=8.1 Hz), 7.38–7.44(3H, m), 6.34(1H, d, J=3.9 Hz), 8.14(1H, dd,J=1.5 and 3.0 Hz). IR(CHCl₃): 3517, 3431, 3361, 3114, 1708, 1654, 1530,1504, 1332, 1151 cm⁻¹. [α]_(D) ²⁴+33.7±0.7°(c=1.003, MeOH) Anal.(C₂₅H₃₁NO₅S₃.0.2H₂O) Calcd.(%): C, 57.16; H, 6.02; N, 2.67; S, 18.31.Found(%): C, 57.09; H, 5.88; N, 2.76; S, 18.15.

Compound Number IV-1

¹H-NMR(CDCl₃) δ: 0.84 and 1.22(each 3H, each s), 1.43(1H, d, J=10.5 Hz),1.53–2.50(14H, m), 4.09(1H, m), 5.30–5.41(2H, m), 6.17 (1H, d, J=8.7 Hz)6.33 and 7.16(each 2H, each t-like), 7.40 and 7.57 (each 1H, each d,each J=3.9 Hz). IR(CHCl₃): 3514, 3432, 3144, 3102, 1708, 1657, 1531,1506, 1456, 1384, 1167 cm⁻¹. [α]_(D) ²³−45.4±0.9°(c=1.010, MeOH) Anal.(C₂₅H₃₀N₂O₅S₂.0.3H₂O) Calcd.(%): C, 59.10; H, 6.07; N, 5.51; S, 12.62.Found(%): C, 59.12; H, 5.83; N, 5.53; S, 12.41.

Compound Number IV-47

¹H-NMR(CDCl₃) δ: 0.85 and 1.22(each 3H, each s), 1.44(1H, d, J=10.2 Hz),1.54–2.51(14H, m), 4.10(1H, m), 5.31–5.41(2H, m), 6.21 (1H, d, J=8.4Hz), 7.11(1H, dd, J=3.9 and 4.8 Hz), 7.44 and 7.63 (each 1H, each d,each J=3.9 Hz), 7.70(1H, dd, J=1.2 and 4.8 Hz), 7.75 (1H, dd, J=1.2 and3.9 Hz). IR(CHCl₃): 3517, 3423, 3366, 3097, 2665, 1708, 1655, 1530,1505, 1335, 1153 cm⁻¹. [α]_(D) ²³−46.4±0.9°(c=1.010, MeOH) Anal.(C₂₅H₃₁NO₅S₃.0.3H₂O) Calcd.(%): C, 56.97; H, 6.04; N, 2.66; S, 18.25.Found(%): C, 57.10; H, 5.96; N, 2.70; S, 18.02.

Compound Number V-88

mp.105–106° C.; ¹H-NMR(CDCl₃) δ: 1.06(1H, m), 1.19–1.29(2H, m),1.42–1.47(2H, m), 1.58–1.78(4H, m), 2.00–2.19(5H, m), 2.35(2H, t, J=7.2Hz), 2.52(1H, m), 3.82(1H, m), 4.16(2H, s), 5.30–5.42(2H, m), 5.99(1H,d, J=7.5 Hz), 6.79(1H, dt, J=0.9 and 3.9 Hz), 6.96(1H, dd, J=1.5 and 4.8Hz), 7.05(1H, m), 7.28(1H, dd, J=3.0 and 4.8 Hz), 7.37(1H. d, J=3.9 Hz).IR(KBr): 3367, 2667, 1700, 1612, 1543, 1520, 1317, 1244 cm⁻¹. [α]_(D)²⁴+70.2±1.1°(c=1.006, MeOH) Anal. (C₂₄H₂₉NO₃S₂) Calcd.(%): C, 64.98; H,6.59; N, 3.16; S, 14.46. Found(%): C, 64.92; H, 6.52; N, 3.32; S, 14.48.

Compound Number VI-1

¹H-NMR(CDCl₃) δ: 1.24–2.13(13H, m), 2.22(1H, m), 2.32(2H, t, J=7.2 Hz),3.41(1H, m), 3.44(1H, m), 5.18–5.36(2H, m), 6.19(1H, m), 6.33 and7.15(each 2H, each t, each J=2.4 Hz), 7.28 and 7.55(each 2H, each t,each J=3.9 Hz). IR(CHCl₃): 3512, 3439, 3144, 3100, 1708, 1658, 1535,1508, 1446, 1167 cm⁻¹. [α]_(D) ²⁶+69.5±1.1°(c=1.012, MeOH) Anal.(C₂₃H₂₈N₂O₅S.0.5H₂O) Calcd.(%): C, 56.89; H, 6.02; N, 5.77; S, 13.21.Found(%): C, 56.91; H, 5.96; N, 5.91; S, 13.37.

Compound Number VI-31

¹H-NMR(CDCl₃) δ: 1.18–2.10(13H, m), 2.11(1H, m), 2.21–2.35(2H, m),3.35(1H, m), 3.46(1H, m), 4.12(2H, s), 5.17–5.34(2H, m), 5.88(1H, m),6.74(1H, d, J=3.9 Hz), 7.21–7.38(6H, m). IR(CHCl₃): 3511, 3432, 3065,1708, 1642, 1547, 1515, 1455 cm⁻¹. [α]_(D) ²³30 69.1±1.1°(c=1.009, MeOH)Anal. (C₂₆H₃₁NO₃S.0.1H₂O) Calcd.(%): C, 71.07; H, 7.16; N, 3.19; S,7.30. Found(%): C, 70.91; H, 7.18; N, 3.19; S, 7.34.

Compound Number VI-40

¹H-NMR(CDCl₃) δ: 1.18–2.15(14H, m), 2.24–2.34(2H, m), 3.36(1H, m),3.58(1H, m), 5.19–5.40(2H, m), 6.07(1H, m), 7.28–7.42(3H, m), 7.51(1H,d, J=0.6 Hz), 7.56–7.59(2H, m), 7.72(1H, d, J=0.6 Hz). IR (CHCl₃): 3514,3446, 1709, 1649, 1550, 1520, 1491 cm⁻¹. [α]_(D) ²²+79.4±1.2°(c=1.004,MeOH) Anal. (C₂₅H₂₉NO₃S.0.2H₂O) Calcd.(%): C, 70.29; H, 6.94; N, 3.28;S, 7.51. Found(%): C, 70.26; H, 6.68; N, 3.48; S, 7.44.

Compound Number VI-47

¹H-NMR(CDCl₃) δ: 1.14–2.16(13H, m), 2.23(1H, m), 2.30–2.37(2H, m),3.41(1H, m), 3.45(1H, m), 5.18–5.36(2H, m), 6.19(1H, m), 7.11 (1H, dd,J=3.9 and 5.1 Hz), 7.32 and 7.62(each 1H, each d, each J=3.9 Hz),7.39(1H, dd, J=1.5 and 5.1 Hz), 7.75(1H, dd, J=1.5 and 3.9 Hz).IR(CHCl₃): 3512, 3440, 3096, 1708, 1657, 1534, 1507, 1402, 1336, 1153cm⁻¹. [α]_(D) ²⁵+69.2±1.1°(c=1.006, MeOH) Anal. (C₂₃H₂₇NO₅S₃.0.1H₂O)Calcd.(%): C, 55.57; H, 5.51; N, 2.83; S, 19.42. Found(%): C, 55.55; H,5.32; N, 2.85; S, 19.21.

Compound Number VI-55

¹H-NMR(CDCl₃) δ: 1.18–2.18(13H, m), 2.23(1H, m), 2.31–2.35 (2H, m),2.38(3H, s), 3.43(2H, m), 5.18–5.36(2H, m), 5.98(1H, m), 6.14(1H, m),6.19(1H, t, J=3.3 Hz), 7.17(1H, m), 7.29 and 7.53(each 1H, each d, eachJ=3.9 Hz). IR(CHCl₃): 3512 3440, 3150, 3101, 1708, 1658, 1535, 1508,1375, 1161 cm⁻¹. [α]_(D) ²⁴+30.9±0.7°(c=1.000, MeOH) Anal.(C₂₆H₃₄N₂O₅S₂.0.3H₂O) Calcd.(%): C, 59.58; H, 6.65; N, 5.35; S, 12.24.Found(%): C, 59.57; H, 6.48; N, 5.51; S, 12.22.

Compound Number VI-80

¹H-NMR(CDCl₃) δ: 1.16–2.14(13H, m), 2.23(1H, m), 2.28–2.36(2H, m),3.54–3.46(2H, m), 5.17–5.37(2H, m), 6.14(1H, m), 7.32(1H, d, J=3.9 Hz),7.38–7.44(2H, m), 7.61(1H, d, J=3.9 Hz), 8.15(1H, dd, J=1.2 and 3.0 Hz).IR(CHCl₃): 3508, 3431, 3114, 1708, 1656, 1534, 1508, 1331, 1152, 1102cm⁻¹. [α]_(D) ²⁴+66.5±1.1°(c=1.003, MeOH) Anal. (C₂₃H₂₇NO₅S₃.0.3H₂O)Calcd.(%): C, 55.35; H, 5.57; N, 2.81; S, 19.28. Found(%): C, 55.29; H,5.54; N, 2.85; S, 19.01.

Compound Number VI-104

¹H-NMR(CDCl₃) δ: 1.18–2.14(13H, m), 2.25(1H, m), 2.31–2.39(2H, m),3.32(2H, m), 3.56(1H, m), 4.09(2H, d, J=0.3 Hz), 5.18–5.38(2H, m),5.89(1H, m), 6.68(1H, d, J=3.6 Hz), 6.94(1H, dd, J=3.6 and 5.1 Hz),7.02(1H, dd, J=1.5 and 3.6 Hz), 7.23(1H, d, J=3.6 Hz), 7.35(1H, dd,J=1.5 and 5.1 Hz). IR(CHCl₃): 3514, 3433, 1709, 1645, 1545, 1516, 1458cm⁻¹. [α]_(D) ²³+61.8±1.0°(c=1.008, MeOH) Anal. (C₂₄H₂₉NO₃S₃.0.2H₂O)Calcd.(%): C, 60.14; H, 6.18; N, 2.92; S, 20.07. Found(%): C, 60.08; H,6.11; N, 2.90; S, 20.05.

Compound Number VI-122

¹H-NMR(CDCl₃) δ: 1.06–2.15(13H, m), 2.27(1H, m), 2.28–2.38(2H, m),3.31(1H, m), 3.54(1H, m), 4.24(2H, d, J=0.6 Hz), 5.17–5.36(2H, m),5.87(1H, m), 6.78(1H, d, J=3.6 Hz), 7.21–7.42(6H, m). IR(CHCl₃): 3514,3433, 3062, 2669, 1709, 1643, 1545, 1514 cm⁻¹. [α]_(D)²²+64.3±1.0°(c=1.000, MeOH) Anal. (C₂₆H₃₁NO₃S₂.0.5H₂O) Calcd.(%): C,65.24; H, 6.74; N, 2.93; S, 13.40. Found(%): C, 65.23; H, 6.55; N, 3.00;S, 13.46.

Compound Number VI-123

¹H-NMR(CDCl₃) δ: 1.06–2.15(13H, m), 2.23(1H, m), 2.28–2.38(2H, m),3.35(1H, m), 3.54(1H, m), 5.20(2H, s), 5.19–5.37(2H, m), 5.95(1H, m),6.94–7.04(4H, m), 7.27–7.35(3H, m). IR(CHCl₃): 3514, 3433, 1709, 1647,1599, 1547, 1518, 1495 cm⁻¹. [α]_(D) ²⁴+67.8±1.1°(c=1.008, MeOH) Anal.(C₂₆H₃₁NO₄S.0.2H₂O) Calcd.(%): C, 68.30; H, 6.92; N, 3.06; S, 7.01.Found(%): C, 68.31; H, 6.84; N, 3.16; S, 7.11.

Compound Number VI-124

¹H-NMR(CDCl₃) δ: 1.06–2.14(13H, m), 2.24(1H, m), 2.30–2.37(2H, m),3.31(1H, m), 3.53(1H, m), 4.50(2H, d, J=0.9 Hz), 5.15–5.36(2H, m),5.89(1H, m), 6.65–6.79(3H, m), 6.95(1H, d, J=3.9 Hz), 7.15–7.21 (2H, m),7.33(1H, d, J=3.9 Hz). IR(CHCl₃): 3512, 3440, 1707, 1643, 1603, 1547,1506 cm⁻¹. [α]_(D) ²²+67.3±1.1°(c=1.009, MeOH) Anal. (C₂₆H₃₂N₂O₃S.0.3H₂)Calcd.(%): C, 68.18; H, 7.17; N, 6.20; S, 7.00. Found(%): C, 68.04; H,7.09; N, 6.25; S, 7.02.

Compound Number VI-133

¹H-NMR(CDCl₃) δ: 1.18–1.81(7H, m), 1.85–1.94(2H, m), 2.01–2.13 (2H, m),2.22–2.33(3H, m), 3.41(1H, m), 3.33(1H, m), 3.49(2H, s), 3.54 (1H, m),4.15(2H, s), 5.17–5.37(2H, m), 5.90(1H, m), 6.12(1H, dd, J=0.9 and 3.0Hz), 6.31(1H, dd, J=1.8 and 3.0 Hz), 6.81 and 7.30 (each 1H, each d,each J=3.6 Hz), 7.34(1H, dd, J=0.9 and 1.8 Hz). IR(CHCl₃): 3516, 3433,1709, 1643, 1547, 1516 cm⁻¹. [α]_(D) ²³+71.3±1.1°(c=1.004, MeOH) Anal.(C₂₄H₂₉NO₄S.0.3H₂O) Calcd.(%): C, 66.58; H, 6.89; N, 3.24; S, 7.41.Found(%): C, 66.55; H, 6.63; N, 3.37; S, 7.51.

Compound Number VI-303

¹H-NMR(CDCl₃) δ: 1.18–2.14(13H, m), 2.26(1H, m), 2.31–2.36(2H, m),3.30(1H, m), 3.64(1H, m), 3.82(3H, s), 5.19–5.39(2H, m), 6.06(1H, m),6.89–7.0(6H, m), 7.66(2H, d, J=8.1 Hz). IR(CHCl₃): 3514, 3446, 1709,1649, 1550, 1520, 1491 cm⁻¹. [α]_(D) ²²+76.3±1.2°(c=1.009, MeOH) Anal.(C₂₈H₃₃NO₅.0.2H₂O) Calcd(%): C, 71.99; H, 7.21; N, 3.00. Found(%): C,72.05; H, 7.35; N, 2.93.

The compounds prepared in Examples above were tested for determining thein vivo and in vitro activities according to the method as shown inExperimental examples below.

Experiment 1 Binding Activity to PGD₂ Receptor

(1) Preparation of Human Platelet Membrane Fraction

Blood was collected using a plastic syringe containing 3.8% sodiumcitrate from the vein of healthy volunteers (adult male and female),then put into a plastic test tube and mixed by slow-reversion. Thesample was then centrifuged at 1800 rpm, for 10 min at room temperature,and the supernatant containing PRP (platelet-rich plasma) was collected.The PRP was re-centrifuged at 2300 rpm, for 22 min at room temperatureto obtain platelets. The platelets were homogenized using a homogenizer(Ultra-Turrax) followed by centrifugation 3 times at 20,000 rpm, 10 minat 4° C. to obtain a platelet membrane fraction. After proteindetermination, the membrane fraction was adjusted to 2 mg/ml andpreserved in a refrigerator at −80° C. until using for the binding test.

(2) Binding to PGD₂ Receptor

To a binding-reaction solution (50 mM Tris/HCl, pH 7.4, 5 mM MgCl₂) (0.2ml) were added the human platelet membrane fraction (0.1 mg) and 5 nM[³H]PGD₂ (115 Ci/mmol), and the mixture was reacted at 4° C. for 90 min.After the reaction, the mixture was filtered through a glass fiberfilter paper and washed several times with cooled physiological saline,then the radioactivity retained on the filter paper was measured. Thespecific-binding ratio was calculated by subtracting the non-specificbinding ratio which is the radioactivity similarly measured in thepresence of 10 μM PGD₂ from the total binding. The inhibitory activityof each compound was expressed as the concentration required for 50%inhibition (IC₅₀), which was determined by depicting a substitutioncurve by plotting the binding ratio (%) in the presence of eachcompound, where the binding ratio in the absence of a test compound is100%.

Experiment 2 Binding Activity to TXA₂ Receptor

(1) Preparation of Human Platelet Membrane Fraction

The human platelet membrane fraction was prepared in accordance withExperiment 1 (1).

(2) Binding to TXA₂ Receptor

To a binding-reaction solution (50 mM Tris/HCl, pH 7.4, 10 mM MgCl₂)(0.2 ml) were added the human platelet membrane fraction (0.05 mg) and 2nM Sodium[³H](+)-(5Z)-7-[3-endo-[(phenylsulfonyl)amino]bicyclo[2.2.1]hept-2-exo-yl]heptenoate(Japanese Patent Publication (Kokoku) No.79060/1993, hereinafterreferred to as (+)-S-145 sodium salt) (26.4 Ci/mmol), and the mixturewas reacted at room temperature for 90 min. After the reaction, theresultant mixture was filtered through a glass fiber filter paper andwashed several times with cooled physiological saline, then theradioactivity retained on the filter paper was measured. Thespecific-binding ratio was calculated by subtracting the non-specificbinding ratio (the radio activity similarly determined in the presenceof 10 μM (+)-S-145 sodium salt) from the total binding. The inhibitoryactivity of each compound was expressed as the concentration requiredfor 50% inhibition (IC₅₀), which was determined by depicting asubstitution curve by plotting the binding ratio (%) in the presence ofeach compound, where the binding ratio in the absence of a test compoundis 100%.

Experiment 3 Evaluation of Antagonistic Activity Against PGD₂ Receptor

Receptor Using Human Platelet

Peripheral blood was collected from a healthy volunteer using a syringein which 1/9 volume of a citric acid/dextrose solution was previouslyadded. The sample was subjected to centrifugation at 1200 rpm for 10 minto obtain the supernatant (PRP: platelet rich plasma). The resultant PRPwas washed 3 times with a washing buffer and the number of platelets wascounted with a micro cell counter. A suspension adjusted to contain theplatelets at a final concentration of 5×10⁸/ml was warmed at 37° C.,then subjected to the pre-treatment with 3-isobutyl-1-methylxanthine(0.5 mM) for 5 min. To the suspension was added a test compound dilutedat various concentration, and 10 minutes later, 0.1 μM PGD₂ was added toinduce the reaction 2 minutes later, hydrochloric acid was added toterminate the reaction. The platelet was destroyed with an ultrasonichomogenizer. After centrifugation, the cAMP in the supernatant wasdetermined by radioimmunoassay. PGD₂ receptor antagonism of a drug wasevaluated as follows: the inhibition rate regarding cAMP increased bythe addition of PGD₂ was determined at each concentration, and theconcentration of the drug required for 50% inhibition (IC₅₀) wascalculated.

The results of Experiment 1–3 are shown below. The results of Experimentof compounds of Example are shown in Table 68 and Table 69 and theresults of Experiment of compounds of Example of reference are shown inTable 70 and Table 71.

TABLE 68 Binding activity Binding activity Inhibitory to PGD₂ receptorto TXA₂ receptor activity for the in human platelet in human plateletincrease of cAMP membrane membrane caused by PGD₂ fraction fraction inhuman platelet Compd. No.. IC₅₀(μM) IC₅₀(μM) IC₅₀(μM) I-5A-59a 0.0110.079 I-7A-1a 0.0076 0.0046 0.035 I-7A-31a 0.063 0.057 I-7A-47a 0.0730.003 0.018 I-7A-59a 0.0098 0.012 I-7A-88a 0.034 0.036 I-7A-104a 0.0240.082 I-7A-143a 0.084 0.036 I-7I-1a 0.0026 0.064 I-7I-31a 0.065 0.092I-7I-47a 0.0012 0.085 I-7I-88a 0.033 0.025 I-71-126a 0.061 0.021I-71-270a 0.0009 0.026 I-7I-307a 0.051 0.097 I-7M-1e 0.044 0.039I-7M-59a 0.040 0.024 I-7M-143a 0.021 0.026 I-7M-270a 0.0014 0.012I-7M-307a 0.100 0.024 I-7M-315a 0.039 0.028 I-7M-316a 0,062 0.11I-7M-317a 0.074 0.018 I-7M-318a 0.068 0.028 I-7M-333a 0.013 0.094I-7M-337a 0.037 0.019 I-7M-343a 0.029 0.033 I-7M-393a 0.019 0.11I-7M-424a 0.0076 0.02 I-7M-446a 0.0063 0.027 I-7P-1a 0.034 0.036 I-7R-1a0.01 0.018 I-7R-270a 0.012 0.027

TABLE 69 Binding activity Binding activity Inhibitory to PGD₂ receptorto TXA₂ receptor activity for the in human platelet in human plateletincrease of cAMP membrane membrane caused by PGD₂ fraction fraction inhuman platelet Compd. No.. IC₅₀(μM) IC₅₀(μM) IC₅₀(μM) II-5A-1a 0.0270.0012 0.066 II-5A-31a 0.013 0.045 II-5A-55a 0.0053 0.0006 0.017II-5A-88a 0.022 0.019 II-5A-104a 0.013 0.047 II-5A-143a 0.047 0.024II-5B-55a 0.0042 0.0012 0.011 II-5F-55a 0.0019 0.061 II-6A-55a 0.0470.026 0.1 II-7A-31a 0.082 0.027 II-7A-47a 0.0038 0.059 II-7A-55a 0.00620.0042 0.057 II-7A-55e 0.019 0.19 II-7A-59a 0.040 0.042 II-7A-143a 0.0370.019 II-7I-55a 0.0018 0.0023 0.063 II-7I-59a 0.015 0.015 II-7I-126a0.102 0.013 II-7I-239a 0.046 0.042 II-7I-270a 0.0006 0.032 II-7I-343a0.0041 0.079 II-7M-1a 0.0012 0.054 II-7M-1e 0.011 0.12 II-7M-1k 0.0200.02 II-7M-31a 0.047 0.033 II-7M-47a 0.024 0.0018 0.073 II-7M-55a 0.00130.0022 0.013 II-7M-59a 0.027 0.021 II-7M-88a 0.122 0.014 II-7M-126a0.119 0.026 II-7M-197a 0.012 0.019 II-7M-239a 0.055 0.028 II-7M-270a0.0006 0.034 II-7M-307a 0.077 0.021 II-7M-332a 0.0017 0.067 II-7M-343a0.0045 0.075 II-7N-55a 0.0065 0.0025 0.02 II-7P-55a 0.0084 0.047II-7R-55a 0.0036 0.013 II-7R-270a 0.015 0.023 II-7U-55a 0.021 0.077

TABLE 70 Binding activity Binding activity Inhibitory to PGD₂ receptorto TXA₂ receptor activity for the in human platelet in human plateletincrease of cAMP membrane membrane caused by PGD₂ fraction fraction inhuman platelet Compd. No.. IC₅₀(μM) IC₅₀(μM) IC₅₀(μM) I-1 0.0043 0.0030.0013 I-10 0.0016 0.092 0.0018 I-31 0.0082 0.130 0.0057 I-47 0.00410.0062 0.007 I-59 0.00041 0.016 0.0046 I-66 0.0046 0.034 0.044 I-790.00042 0.015 0.024 I-80 0.0066 0.0052 0.039 I-82 0.032 0.0018 0.053I-88 0.0076 0.078 0.0047 I-93 0.0070 0.072 0.0084 I-94 0.001 0.083 0.01I-104 0.0001 0.039 0.0016 I-106 0.013 0.013 0.0093 I-117 0.0091 0.00380.047 I-128 0.020 0.048 0.01 I-129 0.011 0.052 0.022 I-131 0.044 0.0190.041 I-132 0.032 0.012 0.043 I-136 0.023 0.016 0.015 I-143 0.0027 0.0280.0019 I-146 0.044 0.019 0.073 I-160 0.028 0.02 0.085 I-168 0.000460.034 0.029 I-169 0.00061 0.032 0.026 I-170 0.00092 0.027 0.017 I-1820.061 0.028 0.011.

TABLE 71 Binding activity Binding activity Inhibitory to PGD₂ receptorto TXA₂ receptor activity for the in human platelet in human plateletincrease of cAMP membrane membrane caused by PGD₂ fraction fraction inhuman platelet Compd. No.. IC₅₀(μM) IC₅₀(μM) IC₅₀(μM) II-1 0.002 0.0120.011 II-18 0.0079 0.030 0.0003 II-37 0.026 0.0043 0.035 II-47 0.000960.0036 0.004 II-55 0.0015 0.0044 0.0039 II-59 0.0001 0.014 0.024 II-1010.072 0.0040 0.045 II-117 0.022 0.0026 0.024 II-126 0.0046 0.045 0.004II-138 0.032 0.072 0.025Experiment 4 Change of Plasma Concentration of Drug in Rat

Compound (0.5 to 2 mg/kg) was administered intravenously to Jcl-SD malerats. The concentration of the unchanged compound was measured at 2, 5,15, 30, 60, 120, and 240 min after the administration by the use of HPLC(determination limit; 0.05 μg/ml) and LC/MS/MS (determination limit;0.001 μg/ml) and the half life of the disappearance was calculated.

TABLE 72 half life of the disappearance Compd. No.. (min) ReferenceCompd.I-1 9.4 I-7M-1a 26.3 Reference Compd.I-143 4.7 I-7M-143a 38.4Reference Compd.II-59 11.0 II-7I-59a 67.0 II-7M-59a 92.6

A half-life of the disappearance of a compound of the present inventionwas observed to be about 3 to 8 times as long as that of the compound ofreference and the metabolic stability was confirmed.

Experiments for comparing the present compound having a dualantagonistic activity against PGD₂/TXA₂ receptors (e.g., II-7I-55a,II-7M-55a) with a PGD₂ receptor antagonist (e.g., B-1, B-2) and a TXA₂antagonist (e.g., A) are shown below.

The experiments were carried out in accordance with the above Experiment1–3 for the purpose of comparing the compound having a dual antagonisticactivity against PGD₂/TXA₂ receptor with a PGD₂ receptor antagonist anda TXA₂ receptor antagonist.

TABLE 73 Experiment 1 Experiment 2 Experiment 3 AntagonisticAntagonistic Antagonistic activity activity activity against PGD₂against TXA₂ against PGD₂ receptor receptor receptor Compd. IC₅₀ (μM)IC₅₀ (μM) IC₅₀ (μM) Compound 0.0018 0.0023 0.063 (II-7I-55a) Compound0.0013 0.0022 0.013 (II-7M-55a) TXA₂ receptor >10 0.0038 >10 antagonist(A) PGD₂ receptor 0.022 0.37 0.030 antagonist (B-1)Comparative Experiment 2Antigen-Induced Bronchial Hyperresponsiveness

Male Hartley guinea pigs were actively sensitized to ovalbumin (OVA) byinhalation of aerosolized solution of 1% ovalbumin twice at a weekinterval. One week after the second sensitization, the animals weretreated with antihistamine, diphenhydramine (10 mg/kg, i.p.), and thenchallenged with 1% OVA aerosol for 5 min. Twenty four hours later,acetylcholine at doses at 3.13, 6.25, 12.5, 25, 50 and 100 micro g/kgwas sequentially injected into the animals which were anesthetized withpentobarbital (30 mg/kg, i.p.). The bronchoconstriction induced by eachdose of acetylcholine was monitored by the modified method ofKonzett-Rössler technique, and made a dose-response curve ofacetylcholine. Using the dose-response curve, the dose required for 200%increase in bronchoconstriction from baseline (PD₂₀₀) was calculated ineach animal and used as an indication of bronchial responsiveness.Compounds were orally administered 1 hour before antigen challenge. **:P<0.01 vs Vehicle(Dunnett's test), ^(##): P<0.01 vs Vehicle(Student's ttest).

TABLE 74 Log PD₂₀₀ Vehicle 1.033 ± 0.053 Compound (II-7I-55a)10 mg/kg1.442 ± 0.055** Compound (II-7M-55a)10 mg/kg 1.485 ± 0.119** Negativecontrol 1.517 ± 0.067^(##)

TABLE 75 Log PD₂₀₀ Vehicle 1.125 ± 0.023 Compound (B-2)10 mg/kg 1.237 ±0.052 Negative control 1.465 ± 0.074^(##)

TABLE 76 Log PD₂₀₀ Vehicle 1.11 ± 0.06 Compound (A)1 mg/kg 1.29 ± 0.04Compound (A)10 mg/kg 1.61 ± 0.09** Negative control 1.69 ± 0.06^(##)

As shown in Table 74 to Table 76, a PGD₂ receptor antagonist (B-2) didnot inhibit the induction of bronchial hyperresponsiveness, but TXA₂receptor antagonist (A) and PGD₂/TXA₂ dual receptor antagonist, (e.g.,II-71-55a, II-7M-55a) suppressed it, indicating that TXA₂ receptorantagonism is necessary for improvement of bronchialhyperresponsiveness.

Comparative Experiment 3

Antigen-Induced Increase in the Eosinophil Number in BronchoalveolarLavage Fluid.

Bronchoalveolar lavage was performed with 10 mL of saline, after theanimals were sensitized and challenged with antigen. The number of totalcells in the recovered fluid was stained with Türk and counted usinghemocytometer. *: P<0.05, **:P<0.01 vs Vehicle(Dunnett's test), ^(##):P<0.01 vs Vehicle(Student's t test). ( ): inhibition %.

TABLE 77 Total cells (× 10⁶cells/animal) Vehicle 23.36 ± 2.33 Compound(II-7I-55a) 10 mg/kg 12.26 ± 1.54**(80%) Compound (II-7M-55a) 10 mg/kg18.29 ± 1.46 (36%) Negative control  9.43 ± 0.78^(##)

TABLE 78 Total cells (× 10⁶ cells/animal) Vehicle 17.12 ± 2.20 Compound(B-2) 10 mg/kg  9.72 ± 2.32* (53%) Negative control  3.20 ± 0.52^(##)

TABLE 79 Total cells (× 10⁶ cells/animal) Vehicle 13.89 ± 2.42 Compound(A) 10 mg/kg 15.20 ± 2.20 (−12%) Negative control 2.98 ± 0.28^(##)

As shown in Table 77 to Table 79, PGD₂ receptor antagonist (B-2) andPGD₂/TXA₂ dual receptor antagonist (II-71-55a, II-7M55a) significantlysuppressed the eosinophil infiltration. But a TXA₂ receptor antagonist(A) did not show any inhibitory actions. These results indicate thatPGD₂ receptor antagonism is necessary for suppression of inflammatorycell infiltration.

Comparative Experiment 4

Acceleration of Vascular Permeability of Conjunctiva Induced by PGD₂ andU-46619

Using male Hartley guinea pigs, PGD₂- and TxA₂ receptor-mediatedincrease in conjunctival vascular permeability was produced byinstillation of each 10 μl solution of either 0.1% PGD₂ or U-46619 (TXA₂receptor agonist) to the both eyes without anesthetization. Immediatelyafter that, Evans blue dye (20 mg/kg) was intravenously injected. 30 minafter the challenge, guinea pigs were sacrificed by bleeding underanesthesia with Pentobarbital (30 mg/kg, i.p.) and the tissue ofconjunctiva was removed. The dye leaked into the tissue was extracted informamide 3 ml at 60° C. for more than 24 h, and then centrifuged. Theabsorbance of the supernatant was measured at 620 nm. The amount of dyewas calculated from the calibration curve of Evans blue dye. Eachcompound was suspended in 0.5% methyl-cellulose and administrated orallyat 1 h before the challenge. The antagonistic activity was evaluated bythe inhibition ratio against the dye leaked into conjunctiva caused byPGD2 or U-46619 at each dose and then a 50% effective dose of inhibition(ED₅₀ value) of each compound was calculated.

TABLE 80 ED₅₀ (mg/kg) Compound PGD₂ TXA₂ (U-46619) II-7I-55a 0.33 0.030II-7M-55a 0.043 0.083 PGD₂ receptor antagonist 0.099 >10 (B-2) TXA₂receptor antagonist >30 0.017 (A)

As shown in Table 80, a PGD₂ receptor antagonist (B-2) inhibited theincrease in vascular permeability in conjunctiva by the stimulation withPGD₂ but did not inhibit that caused by U-46619, viceversa, a TXA2receptor antagonist (A) suppressed only U-46619-induced response.PGD₂/TXA₂ dual receptor antagonist (e.g., II-7I-55a, II-7M-55a) showedboth responses. Thus, the inhibition of both receptor-mediated responseswas ascertained in vivo.

Formulation Example

It is to be noted that the following Formulation Examples 1 to 8 aremere illustration, but not intended to limit the scope of the invention.The term “Active ingredient” means a compound of the present invention,the prodrug thereof, their pharmaceutically acceptable salt, or theirhydrate.

Formulation Example 1

Hard gelatin capsules are prepared using the following ingredients:

Dose (mg/capsule) Active ingredient 250 Starch, dried 200 Magnesiumstearate  10 Total 460 mg

Formulation Example 2

Tablet are prepared using the following ingredients:

Dose (mg/tablet) Active ingredient 250 Cellulose, microcrystals 400Silicon dioxide, fumed  10 Stearic acid  5 Total 665 mg

The ingredients are blended and compressed to form tablets each weighing665 mg.

Formulation Example 3

An aerosol solution is prepared containing the following components:

Weight Active ingredient 0.25 Ethanol 25.75 Propellant 22(chlorodifluoromethane) 74.00 Total 100.00

The active ingredient is mixed with ethanol and the admixture added to aportion of the propellant 22, cooled to −30° C. and transferred to afilling device. The required amount is then fed to a stainless steelcontainer and diluted with the reminder of the propellant. The valveunits are then fitted to the container.

Formulation Example 4

Tablets, each containing 60 mg of active ingredient, are made asfollows.

Active ingredient 60 mg Starch 45 mg Microcrystals cellulose 35 mgPolyvinylpyrrolidone (as 10% solution in 4 mg water) Sodiumcarboxymethyl starch 4.5 mg Magnesium stearate 0.5 mg Talc 1 mg Total150 mg

The active ingredient, starch, and cellulose are passed through a No. 45mesh U.S. sieve, and the mixed thoroughly. The aqueous solutioncontaining polyvinylpyrrolidone is mixed with the resultant powder, andthe admixture then is passed through a No. 14 mesh U.S. sieve. Thegranules so produced are dried at 50° C. and passed through a No. 18mesh U.S. sieve. The sodium carboxymethyl starch, magnesium stearate,and talc, previously passed through No. 60 mesh U.S. sieve, are thenadded to the granules which, after mixing, are compressed on a tabletmachine to yield tablets each weighing 150 mg.

Formulation Example 5

Capsules, each containing 80 mg of active ingredient, are made asfollows:

Active ingredient 80 mg Starch 59 mg Microcrystals cellulose 59 mgMagnesium stearate 2 mg Total 200 mg

The active ingredient, cellulose, starch, and magnesium stearate areblended, passed through a No. 45 mesh U.S. sieve, and filled into hardgelatin capsules in 200 mg quantities.

Formulation Example 6

Suppositories, each containing 225 mg of active ingredient, are made asfollows:

Active ingredient  225 mg Saturated fatty acid glycerides 2000 mg Total2225 mg

The active ingredient; is passed through a No. 60 mesh U.S. sieve andsuspended in the saturated fatty acid glycerides previously melted usingthe minimum heat necessary. The mixture is then poured into asuppository mold of nominal 2 g capacity and allowed to cool.

Formulation Example 7

Suspensions, each containing 50 mg of active ingredient per 5 ml dose,are made as follows:

Active ingredient 50 mg Sodium carboxymethyl cellulose 50 mg Syrup 1.25ml Benzoic acid solution 0.10 ml Flavor q.v. Color q.v. Purified waterto total 5 ml

The active ingredient is passed through a No. 45 U.S. sieve, and mixedwith the sodium carboxymethyl cellulose and syrup to form a smoothpaste. The benzoic acid solution, flavor and color are diluted with aportion of the water and added, with stirring. Sufficient water is thenadded to produce the required volume.

Formulation Example 8

An intravenous formulation may be prepared as follows:

Active ingredient  100 mg Isotonic saline 1000 ml

The solution of the above ingredients is generally administeredintravenously to a subject at a rate of 1 ml per minute.

INDUSTRIAL APPLICABILITY

The pharmacological effect of the compound of the present invention iscompared with that of TXA₂ receptor antagonist and PGD₂ receptorantagonist in the following table.

TABLE 81 TXA₂ receptor PGD₂ receptor antagonist antagonist Compound (I)Bronchial asthma Eosinophilic x ⊚ ⊚ infiltration Advance of respiratory⊚ x ⊚ anaphylaxis Respiratory ⊚ x ⊚ contraction

In bronchial asthma, a TXA₂ receptor antagonist itself can inhibitadvance of respiratory anaphylaxis and respiratory contraction, but hasno effect for eosinophilic infiltration. A PGD₂ receptor antagonistitself can inhibit eosinophilic infiltration, but has no effect foradvance of respiratory anaphylaxis and respiratory contraction. On theother hand, a compound having a dual antagonistic activity againstPGD₂/TXA₂ receptors like the compound (I) is efficient for all ofeosinophilic infiltration, advance of respiratory anaphylaxis andrespiratory contraction.

A TXA₂ receptor antagonist has no effect for eosinophilic infiltrationbut was ascertained to increase the inhibitory effect for eosinophilicinfiltration caused by a PGD₂ receptor antagonist. That is, a TXA₂receptor antagonist and a PGD₂ receptor antagonist were ascertained toshow a synergistic effect. Then, a compound having a dual antagonisticactivity against PGD₂/TXA₂ receptors like the compound (I) is veryefficient.

The compound having a dual antagonistic activity against PGD₂/TXA₂receptors is useful for treating systemic mastocytosis and disorder ofsystemic mast cell activation as well as tracheal contraction, asthma,allergic rhinitis, allergic conjunctivitis, urticaria, itching, atopicdermatitis, alimentary allergy, ischemic reperfusion injury,cerebrovascular disorder, and inflammation, and effective for treatingor improving condition of diseases such as arteriosclerosis, myocardialinfarction, acute myocardial ischemia angina, cardiovascular shock orpreventing unexpected death and the like, especially asthma or nasalblockage.

With a dual antagonistic activity against both a TXA₂ receptor and aPGD₂ receptor, the present compound can overcome some problems such asthat due to the metabolic rate difference of each compound, which occurupon simultaneous administration of both a TXA₂ receptor antagonist anda PGD₂ receptor antagonist.

1. A compound of the formula (I):

A is alkylene optionally intervened with a heteroatom, optionally havingan oxo group, optionally substituted with halogen and/or optionallyhaving an unsaturated bond; R is —C(═O)—R¹, —CH₂—R¹, or tetrazolyl; R¹is hydroxy, alkyloxy, or optionally substituted amino; m is 0 or 1;provided that combinations wherein m is 1, A is —CH═CH—CH₂—CH₂—CH₂— andR is —C(═O)—R¹ (R¹ is hydroxy or alkyloxy) or wherein A is—CH₂—CH═CH—CH₂—CH₂—CH₂— and R is —C(═O)—R¹ wherein R¹ is hydroxy oralkyloxy are excluded, p is 0 or 1, provided that when p=0,

X¹ and X³ are each independently optionally substituted aryl, optionallysubstituted heteroaryl or optionally substituted non-aromaticheterocyclyl; X² is a bond, —CH₂—, —CH₂—CH₂—, —C(═O)—, —O—, —S—, —SO—,—SO₂—, —NH—, —N(CH₃)—, —C(═N—O—CH₃)—, —N═N—, —CH═CH—, —(C═O)—NH—,—NH—(C═O)—, —CH₂—NH—, —NH—CH₂—, —CH₂—O—, —O—CH₂—, —CH₂—S, —S—CH₂—,—CH₂—SO₂—, —SO₂—CH₂—, —SO₂—NH—, —NH—SO₂—, —C(═CH₂)—, —SO₂N(Me)—,—CH₂NHSO₂—, —CH₂NH—(C═O)—, —NH—C(═O)—NH or —NH—C(═O)—N(Me)—; X⁴ is—CH₂—, —CH₂—CH₂—, —C(═O)—, —SO—, —SO₂—, —(C═O)—NH—, —NH—(C═O)—,—CH₂—NH—, —NH—CH₂—, —CH₂—O—, —O—CH₂—, —CH₂—S—, —S—CH₂—, —CH₂—SO₂—,—SO₂—CH₂—, —SO₂—NH— or —NH—SO₂—, provided that a combination wherein

A is —CH═CH—CH₂—CH₂—CH₂—, R is —COOH, m is 1, p is 0, X¹ and X³ arephenyl, and X² is —N═N—, is excluded and provided that when

X¹ and X³ are phenyl, X² is —CH═CH—, —O—, or —S—, m is 0, and p is 0, acompound wherein A is —CH═CH—CH₂—CH₂—CH₂—C(CH₃)₂— and R is COOH, A is—CH₂—CH═CH—CH₂—CH₂—C(CH₃)₂— and R is COOH, A is—CH₂—C(═O)—CH₂—CH₂—CH₂—CH₂— and R is COOH, A is —CH₂—CH₂—CH₂—CH₂—CH₂—and R is —COOH, A is —CH₂—CH₂—CH₂—CH₂—CH₂—CH₂— and R is —COOH, A is—CH₂—CH═CH—CH₂—CH₂—CH₂— and R is —CH₂OH, or A is —CH═CH—CH₂—CH₂—CH₂— andR is —CH₂OH, is excluded, a pharmaceutically acceptable salt or asolvate thereof.
 2. A compound as described in claim 1 wherein A isalkylene optionally intervened with a heteroatom, optionally having anoxo group, optionally substituted with halogen and/or optionally havingan unsaturated bond; R is —C(═O)—R¹, —CH₂—R¹, or tetrazolyl; R¹ ishydroxy, alkyloxy, or optionally substituted amino; provided thatcompounds wherein A is —CH═CH—CH₂—CH₂—CH₂— and R is —C(═O)—R¹ (R¹ ishydroxy or alkyloxy), or A is —CH₂—CH═CH—CH₂—CH₂—CH₂— and R is —C(═O)—R¹wherein R¹ is hydroxy or alkyloxy are excluded, a pharmaceuticallyacceptable salt or a solvate thereof.
 3. A compound as described inclaim 1, wherein A is alkylene intervened with a heteroatom, optionallyhaving an oxo group, optionally substituted with halogen and/oroptionally having an unsaturated bond, a pharmaceutically acceptablesalt, or a solvate thereof.
 4. A compound as described in claim 1,wherein A is C1 to C4 or C7 to C9 alkylene optionally intervened with aheteroatom, optionally having an oxo group, optionally substituted withhalogen and/or optionally having an unsaturated bond, a pharmaceuticallyacceptable salt, or a solvate thereof.
 5. A compound as described inclaim 1, wherein A is —CH₂—CH₂—CH₂—, —CH₂—CH₂—CH(F)—, —CH₂CH═CH—,—CH₂—O—CH₂—, —CH₂CH═C(F)—, —CH₂—CH₂—CH₂—CH₂—, —CH₂CH═CH—CH₂—,—CH₂—CH₂—CH═CH—, —CH═CH—CH₂—CH₂—, —CH₂—CH₂—O—CH₂—, —CH₂—CH₂—S—CH₂—,—CH₂—CO—NH—CH₂—, —CH₂—CH₂—CH₂—CH₂—CH₂—, CH₂CH═CH—CH₂—CH₂—,—CH₂—CH₂—CH₂—CH═CH—, —CH₂—CH₂—CH₂—O—CH₂—, —CH₂—CH₂—CH₂—S—CH₂—,—CH₂—CH₂—CO—NH—CH₂—, —CH₂—CH₂—CH₂—CH₂—CH₂—CH₂—,—CH₂—CH₂—CH₂—CH₂—CH₂—CH(Me)—, —CH₂—CH₂—CH₂—CH₂—CH₂—C(Me)₂—,—CH₂—CH₂—CH₂—CH₂—CH₂—CH(F)—, —CH₂—CH═CH—CH₂—CH₂—CH(Me)—,—CH₂—CH═CH—CH₂—CH₂—C(Me)₂—, —CH₂—CH═CH—CH₂—CH₂—CH(F)—,—CH₂—CH₂—CH₂—CH₂—CH═CH—, —CH₂—CH₂—CH₂—CH₂—CH═C(Me)—,—CH₂—CH₂—CH₂—CH₂—C(Me)═CH—, —CH₂—CH₂—CH₂—CH₂—CH═C(F)—,—CH₂—CH₂—CH₂—CH₂—O—CH₂—, —CH₂—CH═CH—CH₂—O—CH₂—, —CH₂—CH═CH—CH₂—S—CH₂—,—CH₂—CH═C(F)—CH₂—O—CH₂—, —CH₂—CH₂—O—CH₂—CH═CH—, —CH₂—CH₂—CH₂—CH₂—S—CH₂—,—CH₂—CH₂—CH₂—CO—NH—CH₂—, —CH₂—CH₂—CH═N—O—CH₂—, —CH₂—CH₂—S—CH₂—CH₂—CH₂—,—CH₂—CH₂—CH₂—CH₂—CH₂—CH₂—CH₂—, —CH₂—CH═CH—CH₂—CH₂—CH₂—CH₂—,—CH₂—CH₂—CH₂—CH₂—CH₂—O—CH₂—, —CH₂—CH₂—CH₂—CH₂—CH₂—CH₂—CH₂—CH₂—, or—CH₂—CH═CH—CH₂—CH₂—CH₂—CH₂—CH₂—, a pharmaceutically acceptable salt, ora solvate thereof.
 6. A compound as described in claim 5, wherein A is—CH₂—CH₂—CH₂—CH₂—, —CH₂—CH₂—CH₂—CH₂—CH═CH—, —CH₂—CH₂—CH₂—CH₂—O—CH₂—,—CH₂—CH═CH—CH₂—O—CH₂—, —CH₂—CH═CH—CH₂—S—CH₂—, or—CH₂—CH₂—CH₂—CH₂—S—CH₂—, a pharmaceutically acceptable salt, or asolvate thereof.
 7. A compound as described in claim 6, wherein A is—CH₂—CH₂—CH₂—CH₂—O—CH₂—, a pharmaceutically acceptable salt, or asolvate thereof.
 8. A compound as described in claim 1, wherein X¹ andX³ are each independently optionally substituted aryl or optionallysubstituted heteroaryl, a pharmaceutically acceptable salt, or a solvatethereof.
 9. A compound as described in claim 8, wherein at least one ofX¹ and X³ is optionally substituted heteroaryl, a pharmaceuticallyacceptable salt, or a solvate thereof.
 10. A compound as described inclaim 9, wherein X¹ and X³ are each independently optionally substitutedheteroaryl, a pharmaceutically acceptable salt, or a solvate thereof.11. A compound as described in claim 9, wherein at least one of X¹ andX³ is optionally substituted thienyl or optionally substitutedbenzothienyl, a pharmaceutically acceptable salt, or a solvate thereof.12. A compound as described in claim 1, wherein X² is a bond, —CH₂—,—S—, —SO₂—, —CH₂—O—, —O—CH₂—, —CH₂—S—, —S—CH₂—, or —NH—C(═O)—NH—, apharmaceutically acceptable salt, or a solvate thereof.
 13. A compoundas described in claim 1, wherein m is 0 and p is 0, a pharmaceuticallyacceptable salt, or a solvate thereof.
 14. A compound as described inclaim 1, wherein R is —C(═O)—R¹ and R¹ is hydroxy, alkyloxy, oroptionally substituted amino, a pharmaceutically acceptable salt, or asolvate thereof.
 15. A pharmaceutical composition containing a compound,a pharmaceutically acceptable salt, or a solvate thereof as described inclaim 1, together with a pharmaceutically acceptable carrier, excipient,solvent or base.
 16. A pharmaceutical composition having a dualantagonistic activity against PGD₂/TXA₂ receptors as described in claim15.
 17. A pharmaceutical composition as described in claim 15, which isused for the treatment of asthma.
 18. A pharmaceutical composition asdescribed in claim 15, which is used for the treatment of nasalblockage.
 19. A pharmaceutical composition as described in claim 15,which is used for the treatment of allergic conjunctivitis.
 20. Apharmaceutical composition as described in claim 15, which is used forthe treatment of allergic rhinitis.
 21. A method for preparing apharmaceutical composition for treating asthma, nasal blockage, allergicconjunctivitis or allergic rhinitis, which comprises mixing a compoundaccording to claim 1 together with a pharmaceutically acceptablecarrier, excipient, solvent or base.
 22. A method for treating nasalblockage, allergic conjunctivitis or allergic rhinitis, which comprisesadministrating a compound as described in claim 1 to a patient in needthereof.
 23. A compound as described in claim 1, wherein A is—CH₂—CH₂—CH(F)—, —CH₂—O—CH₂—, —CH₂CH═C(F)—, —CH₂—CH₂—S—CH₂—,—CH₂—CH₂—CH₂—CH₂—CH₂—CH(Me)—, —CH₂—CH═CH—CH₂—CH₂—CH(Me)—,—CH₂—CH═CH—CH₂—CH₂—C(Me)₂—, CH₂—CH₂—CH₂—CH₂—CH═C(Me)—,—CH₂—CH₂—CH₂—CH₂—C(Me)═CH—, —CH₂—CH₂—CH₂—CH₂—CH═C(F)—,—CH₂—CH₂—CH₂—CH₂—O—CH₂—, —CH₂—CH═CH—CH₂—O—CH₂—, —CH₂—CH═CH—CH₂—S—CH₂—,—CH₂—CH═C(F)—CH₂—O—CH₂—, —CH₂—CH₂—O—CH₂—CH═CH—, —CH₂—CH₂—CH₂—CO—NH—CH₂—,—CH₂—CH₂—CH═N—O—CH₂—, —CH₂—CH₂—CH₂—CH₂—CH₂—O—CH₂—, or—CH₂—CH═CH—CH₂—CH₂—CH₂—CH₂—CH₂—, or pharmaceutically acceptable salt, ora solvate thereof.
 24. A compound as described in claim 1, wherein p is1, a pharmaceutically acceptable salt, or a solvate thereof.